Clinical / approved drugSubcutaneousEvidence 4/5
Abaloparatide is a PTHrP(1-34) analog that agonizes the PTH1 receptor with preference for its transient RG conformation, activating cAMP signaling to stimulate osteoblast-driven new bone formation.
- Class
- Anabolic osteoporosis agent (PTHrP analog)
- Dose ref
- FDA label reference dose: 80 mcg subcutaneously once daily (a labeled dose, not a recommendation)
- Half-life
- Approximately 1-1.7 hours (FDA label)
- Targets
- PTH1 receptor (PTH1R)
Growth hormoneSubcutaneousEvidence 3/5
A soluble ActRIIB-Fc decoy receptor that sequesters myostatin and activin before they reach activin type II receptors, releasing the natural brake on skeletal muscle growth.
- Class
- Soluble ActRIIB-Fc fusion protein (myostatin/activin ligand trap)
- Dose ref
- Investigational only; trials used 0.02-3 mg/kg subcutaneously
- Half-life
- ~10-15 days
- Targets
- Myostatin, Activin
FTPP, prohibitin-targeting peptide
Research onlyWeight lossSubcutaneousEvidence 2/5
Adipotide is a chimeric peptidomimetic whose CKGGRAKDC homing motif binds prohibitin on white-fat blood-vessel endothelium, where its fused D(KLAKLAK)2 segment disrupts mitochondrial membranes to trigger endothelial apoptosis and regression of the fat tissue's blood supply.
- Class
- Pro-apoptotic peptidomimetic (vascular-targeting antiobesity agent)
- Dose ref
- Preclinical/Phase 1 reference only, NOT a recommendation: ~0.43 mg/kg/day subcutaneously for 28 days in obese monkeys; first-in-human Phase 1 started near 0.03 mg/kg/day SC. No approved human dose.
- Half-life
- Not well characterized in humans; dosed once daily by subcutaneous injection in animal and Phase 1 studies
- Targets
- Prohibitin (white adipose tissue endothelium), Annexin A2-prohibitin receptor complex, Mitochondrial membrane (via D(KLAKLAK)2 motif)
Weight lossSubcutaneousEvidence 4/5
Albiglutide is a long-acting GLP-1 receptor agonist made by fusing two DPP-4-resistant copies of modified human GLP-1 to recombinant human albumin, activating the GLP-1 receptor to boost glucose-dependent insulin secretion and suppress glucagon.
- Class
- GLP-1 receptor agonist (albumin-fusion)
- Dose ref
- Per the discontinued Tanzeum label: 30 mg once weekly subcutaneously, increasable to 50 mg once weekly (historical reference, not a recommendation)
- Half-life
- Approximately 5 days (reported terminal estimates ~5-8 days)
- Targets
- GLP-1 receptor
IAPP, islet amyloid polypeptide
Research onlyMetabolic healthSubcutaneousEvidence 3/5
Amylin, co-secreted with insulin from pancreatic beta-cells, activates brainstem amylin receptors (calcitonin receptor paired with RAMPs) to promote satiation, slow gastric emptying, and suppress postprandial glucagon.
- Class
- Amylin receptor agonist (calcitonin peptide family hormone)
- Dose ref
- No established dose for native amylin; it is an endogenous hormone, not a marketed consumer drug. Reference range applies only to the approved analog pramlintide (Symlin), dosed 15-120 mcg subcutaneously before meals per the FDA label (informational, not a recommendation).
- Half-life
- Native human amylin: approximately 13 minutes (short, rapidly degraded by insulin-degrading enzyme and renal clearance)
- Targets
- Amylin receptor AMY1 (CTR+RAMP1), Amylin receptor AMY2 (CTR+RAMP2), Amylin receptor AMY3 (CTR+RAMP3), Calcitonin receptor, Area postrema (brainstem)
Acetyl Hexapeptide-8, Acetyl Hexapeptide-3
Research onlySkin & cosmeticTopicalEvidence 2/5
Argireline's sequence mimics the N-terminal of SNAP-25 and is proposed to compete during SNARE-complex assembly, destabilizing the complex and reducing acetylcholine release to slightly blunt the muscle contractions that form expression lines.
- Class
- Topical cosmetic peptide (SNAP-25/SNARE-mimicking hexapeptide)
- Dose ref
- Cosmetic formulations commonly use roughly 5-10% topically (original studies used a 10% oil-in-water emulsion); this reflects formulation levels and is explicitly not a dosing recommendation.
- Half-life
- No established human pharmacokinetic half-life; applied topically with negligible systemic absorption.
- Targets
- SNAP-25, SNARE complex, Acetylcholine release
Clinical / approved drugIntravenousEvidence 4/5
Atosiban competitively antagonizes the myometrial oxytocin receptor (with affinity also for vasopressin V1a receptors), reducing the intracellular calcium rise and prostaglandin production that drive uterine contractions.
- Class
- Oxytocin receptor antagonist (tocolytic)
- Dose ref
- Label reference (not a recommendation): 6.75 mg IV bolus over ~1 min, then 300 mcg/min infusion for 3 hours, then 100 mcg/min for up to 45 hours; max duration 48 hours
- Half-life
- Biexponential after IV infusion: initial ~0.2 hours, terminal ~1.7 hours
- Targets
- Oxytocin receptor, Vasopressin V1a receptor
Clinical / approved drugIntravenousEvidence 4/5
Bivalirudin is a bivalent direct thrombin inhibitor that reversibly binds both the catalytic active site and the anion-binding exosite of circulating and clot-bound thrombin to block fibrin formation.
- Class
- Direct thrombin inhibitor (parenteral anticoagulant; hirudin-derived peptide)
- Dose ref
- Per the Angiomax FDA label (not a recommendation): IV bolus 0.75 mg/kg followed by 1.75 mg/kg/h infusion for the duration of PCI, with a 0.3 mg/kg supplemental bolus if needed and infusion reduced in renal impairment/dialysis.
- Half-life
- About 25 minutes with normal renal function; roughly 34-57 minutes in renal impairment and about 3.5 hours in dialysis-dependent patients (Angiomax label).
- Targets
- Thrombin (active catalytic site), Thrombin anion-binding exosite (exosite 1)
Body Protection Compound-157
Research onlyHealing & recoverySubcutaneousEvidence 2/5
Derived from human gastric juice. Animal models suggest effects on angiogenesis, tendon healing and GI repair; human clinical data is very limited.
- Class
- Synthetic gastric peptide
- Dose ref
- No human dosing established
- Half-life
- Not well characterized in humans
- Targets
- Multiple pathways (preclinical)
Reproductive & hormoneSubcutaneousEvidence 4/5
Buserelin is a GnRH receptor superagonist that initially stimulates and then, with continuous non-pulsatile exposure, desensitizes pituitary gonadotrophs to suppress LH, FSH and downstream testosterone or estradiol production.
- Class
- GnRH agonist (LHRH analogue)
- Dose ref
- Label/trial reference figures, not recommendations: advanced prostate cancer 500 mcg SC every 8 hours for 7 days, then 200 mcg SC daily or 400 mcg intranasally three times daily; endometriosis 400 mcg intranasally three times daily for up to ~6 months.
- Half-life
- Short elimination half-life, reported around 72-80 minutes (about 1-2 hours) regardless of route.
- Targets
- GnRH/LHRH receptor, Pituitary gonadotrophs, LH, FSH
Weight lossSubcutaneousEvidence 4/5
Long-acting amylin analog that slows gastric emptying and reinforces satiety; studied in combination with semaglutide (CagriSema).
- Class
- Amylin analog
- Dose ref
- Trial doses up to 4.5 mg weekly
- Half-life
- ~7 days
- Targets
- Amylin / CTR
Miacalcin, Fortical, salmon calcitonin
ApprovedClinical / approved drugSubcutaneousEvidence 3/5
Calcitonin activates the calcitonin receptor on osteoclasts to inhibit bone resorption and lower blood calcium, with additional actions on the kidney and gastrointestinal tract.
- Class
- Calcitonin-receptor agonist (peptide hormone analog)
- Dose ref
- Reference label ranges (not recommendations): 100 USP Units/day SC or IM for postmenopausal osteoporosis and symptomatic Paget disease; 4 to 8 USP Units/kg every 6 to 12 hours for hypercalcemia; 200 USP Units/day intranasally for postmenopausal osteoporosis.
- Half-life
- Approximately 1 hour (subcutaneous salmon calcitonin)
- Targets
- Calcitonin receptor, Osteoclasts
Duratocin, Pabal, Lonactene
ApprovedClinical / approved drugIntramuscularEvidence 4/5
Carbetocin is a long-acting synthetic oxytocin analog that acts as an agonist at peripheral oxytocin receptors in the uterine myometrium, producing sustained contractions that reduce postpartum bleeding.
- Class
- Long-acting oxytocin analog (uterotonic)
- Dose ref
- Label/trial reference: single 100 microgram dose (IV over ~1 min after cesarean per Duratocin label; IM after vaginal birth in the CHAMPION trial) - not a recommendation
- Half-life
- Approximately 85-100 minutes (vs ~3.5 minutes for oxytocin)
- Targets
- Oxytocin receptor (myometrium)
Reproductive & hormoneSubcutaneousEvidence 4/5
Cetrorelix competitively blocks pituitary GnRH receptors, immediately and reversibly suppressing LH and FSH release to prevent a premature LH surge without the initial flare seen with GnRH agonists.
- Class
- GnRH antagonist (synthetic decapeptide)
- Dose ref
- Reference label regimens (not recommendations): 0.25 mg subcutaneously every 24 hours during the late follicular phase, or a single 3 mg subcutaneous dose providing at least 4 days of action.
- Half-life
- Median ~5 hours after a single 0.25 mg dose and ~62.8 hours after a single 3 mg dose (Cetrotide label)
- Targets
- GnRH receptor, Pituitary gonadotrophs, Luteinizing hormone (LH), Follicle-stimulating hormone (FSH)
Growth hormoneSubcutaneousEvidence 3/5
Long-acting growth-hormone-releasing hormone analog. The DAC variant binds serum albumin to extend half-life and sustain GH/IGF-1 elevation.
- Class
- GHRH analog (with or without DAC)
- Dose ref
- 1–2 mg weekly (DAC, research)
- Half-life
- ~6–8 days (DAC)
- Targets
- GHRH receptor
LongevityIntranasalEvidence 2/5
Colivelin simultaneously activates an ADNF-mediated CaMKIV pathway and a Humanin-mediated JAK2/STAT3 pathway to suppress neuronal death in cell and rodent models.
- Class
- Synthetic neuroprotective hybrid peptide (ADNF + Humanin derivative)
- Dose ref
- No established human dose; preclinical rodent studies used roughly 10 pmol to 1 nmol given intracerebroventricularly, plus intraperitoneal and intranasal experiments (research figures only, not recommendations).
- Half-life
- Not established in humans; expected to be short as an unmodified peptide.
- Targets
- Humanin receptor / JAK2-STAT3 pro-survival pathway, ADNF / Ca2+-calmodulin-dependent protein kinase IV (CaMKIV) pathway
polypeptide cortical fraction
Research onlyCognitiveIntramuscularEvidence 2/5
Cortexin is a low-molecular-weight polypeptide fraction from animal cerebral cortex proposed to act as a multi-target neuroprotectant by modulating glutamate (AMPA, kainate, mGluR) and GABA-A receptors, inhibiting brain caspase-8, and influencing neurotrophic and antioxidant pathways.
- Class
- Animal-derived polypeptide neuroprotective bioregulator (brain peptide hydrolysate)
- Dose ref
- Reference only (not a recommendation): Russian clinical use describes intramuscular injection of the reconstituted lyophilizate as a short daily course (commonly ~10 days) with separate adult and pediatric strengths; preclinical models used ~0.5 mg/kg IM.
- Half-life
- Not established; as a multi-component peptide hydrolysate it has no well-characterized human elimination half-life
- Targets
- AMPA receptor, kainate receptor, mGluR1, mGluR5, GABA-A receptor, caspase-8
CognitiveIntranasalEvidence 2/5
Davunetide binds microtubule end-binding proteins to promote microtubule stability and the tau-microtubule interaction, reducing tau hyperphosphorylation in preclinical models.
- Class
- ADNP-derived microtubule-stabilizing neuroprotective peptide
- Dose ref
- Investigational; no approved dose. Trial regimens (not recommendations) used intranasal NAP roughly 5-15 mg in MCI studies and 30 mg twice daily in the phase 2/3 PSP trial.
- Half-life
- Short; preclinical estimates of roughly 15 minutes in brain after intranasal dosing. Human pharmacokinetics were not characterized in the pivotal PSP trial.
- Targets
- Microtubules, Tubulin, Microtubule end-binding proteins EB1/EB3, Tau protein
Reproductive & hormoneSubcutaneousEvidence 5/5
Degarelix competitively and reversibly blocks pituitary GnRH receptors, immediately reducing LH and FSH release and thereby suppressing testosterone without the initial flare seen with GnRH agonists.
- Class
- GnRH receptor antagonist (synthetic decapeptide)
- Dose ref
- Label reference (not a recommendation): 240 mg subcutaneous starting dose (two 120 mg injections), then 80 mg subcutaneous maintenance every 28 days
- Half-life
- ~43 days terminal half-life after the 240 mg starting depot; ~28-29 days for the 80 mg maintenance dose (depot-driven)
- Targets
- Pituitary GnRH receptor, Luteinizing hormone (LH), Follicle-stimulating hormone (FSH), Testosterone
Clinical / approved drugIntranasalEvidence 5/5
Desmopressin selectively stimulates renal V2 vasopressin receptors to increase water reabsorption (antidiuresis) while also triggering release of factor VIII and von Willebrand factor from vascular endothelium.
- Class
- Synthetic vasopressin (V2 receptor) analog; antidiuretic and hemostatic peptide
- Dose ref
- Reference ranges from labels (not recommendations): central diabetes insipidus intranasal 10-40 mcg/day or oral 0.1-1.2 mg/day divided; primary nocturnal enuresis oral 0.2-0.6 mg at bedtime; nocturia (sublingual) 27.7 mcg women / 55.3 mcg men at bedtime; bleeding disorders IV 0.3 mcg/kg over 15-30 minutes.
- Half-life
- Roughly 1.5-3.5 hours depending on route (terminal half-life about 2.8 hours after IV dosing; ~3.3-3.5 hours intranasal)
- Targets
- Vasopressin V2 receptor
Weight lossSubcutaneousEvidence 5/5
Dulaglutide is a long-acting GLP-1 receptor agonist that stimulates glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying and reduces appetite.
- Class
- GLP-1 receptor agonist (Fc-fusion peptide)
- Dose ref
- FDA label (not a recommendation): 0.75 mg, 1.5 mg, 3 mg or 4.5 mg subcutaneously once weekly
- Half-life
- Approximately 5 days
- Targets
- GLP-1 receptor
Weight lossSubcutaneousEvidence 4/5
An exendin-4-based GLP-1 receptor agonist conjugated to an antibody Fc fragment that slows clearance and activates the GLP-1 receptor to boost glucose-dependent insulin secretion, slow gastric emptying and reduce appetite.
- Class
- GLP-1 receptor agonist (exendin-4-based)
- Dose ref
- Studied in trials at 4 mg or 6 mg once weekly subcutaneously (also 2 mg in dose-ranging); reference ranges from research only, not a recommendation or approved dose.
- Half-life
- Approximately 5.6 to 7.5 days (single-ascending-dose pharmacokinetic studies)
- Targets
- GLP-1 receptor
Clinical / approved drugSubcutaneousEvidence 4/5
Enfuvirtide binds the HR1 region of the HIV-1 gp41 envelope subunit and blocks the six-helix bundle conformational change required for fusion of the viral and host cell membranes.
- Class
- HIV-1 gp41 fusion inhibitor (antiretroviral)
- Dose ref
- Per FDA label (reference only, not a recommendation): adults 90 mg subcutaneously twice daily; pediatric patients 2 mg/kg twice daily up to a 90 mg maximum.
- Half-life
- Approximately 3.8 hours (mean 3.8 ± 0.6 h after a single 90 mg subcutaneous dose, per FDA label)
- Targets
- HIV-1 gp41 HR1 (N-terminal heptad repeat), viral envelope glycoprotein gp41
Clinical / approved drugIntravenousEvidence 5/5
Eptifibatide reversibly blocks the platelet GP IIb/IIIa receptor, preventing fibrinogen and von Willebrand factor from cross-linking platelets and thereby inhibiting the final common pathway of platelet aggregation.
- Class
- Glycoprotein IIb/IIIa receptor inhibitor (antiplatelet)
- Dose ref
- Reference (label/trials, not a recommendation): ACS 180 mcg/kg IV bolus then 2 mcg/kg/min infusion up to 72-96h; PCI 180 mcg/kg bolus, 2 mcg/kg/min infusion, plus a second 180 mcg/kg bolus 10 min later; reduced infusion in renal impairment.
- Half-life
- Approximately 2.5 hours (plasma elimination); platelet function recovers about 4-8 hours after stopping the infusion.
- Targets
- Platelet glycoprotein IIb/IIIa receptor (integrin alpha-IIb beta-3)
Byetta, Bydureon, exendin-4
ApprovedWeight lossSubcutaneousEvidence 5/5
Exenatide activates the GLP-1 receptor to increase glucose-dependent insulin secretion, suppress inappropriate glucagon release, and slow gastric emptying.
- Class
- GLP-1 receptor agonist (incretin mimetic)
- Dose ref
- Reference label doses (not recommendations): Byetta 5-10 mcg subcutaneously twice daily before meals; Bydureon BCise 2 mg subcutaneously once weekly
- Half-life
- Approximately 2.4 hours for immediate-release Byetta; extended-release (Bydureon BCise) microspheres release over weeks and exenatide can persist about 10 weeks after the last dose
- Targets
- GLP-1 receptor
Ganirelix acetate, Orgalutran, Antagon
ApprovedReproductive & hormoneSubcutaneousEvidence 4/5
Ganirelix competitively blocks GnRH receptors on pituitary gonadotrophs, producing rapid, reversible suppression of LH and FSH secretion without an initial stimulatory flare.
- Class
- GnRH antagonist (synthetic decapeptide)
- Dose ref
- Label dose of 0.25 mg subcutaneously once daily during the mid-to-late follicular phase until ovulation is triggered (a label figure, not a recommendation)
- Half-life
- About 12.8 hours after a single 0.25 mg dose; roughly 16.2 hours at steady state with daily dosing (label)
- Targets
- GnRH receptor, Pituitary gonadotroph, Luteinizing hormone (LH), Follicle-stimulating hormone (FSH)
LongevitySubcutaneousEvidence 2/5
Naturally occurring tripeptide bound to copper. Studied for wound healing, skin remodeling and gene-expression effects related to tissue repair.
- Class
- Copper peptide complex
- Dose ref
- Topical cosmetic ranges; no systemic dosing established
- Half-life
- Hours
- Targets
- Copper transport / fibroblast signaling
Growth hormoneIntravenousEvidence 3/5
GHRP-2 is a synthetic hexapeptide ghrelin mimetic that activates the growth hormone secretagogue receptor (GHS-R1a) at the hypothalamus and pituitary, amplifying GHRH and reducing somatostatin tone to drive a transient growth hormone pulse.
- Class
- Growth hormone secretagogue / ghrelin receptor (GHS-R1a) agonist (synthetic hexapeptide)
- Dose ref
- Diagnostic use only (not a therapeutic recommendation): single 100 microgram IV bolus in adults, or ~2 micrograms/kg IV in children, for GH-deficiency provocative testing
- Half-life
- Short; GH response peaks ~15-60 min after IV dosing and clears within a few hours (precise human half-life not consistently reported)
- Targets
- Growth hormone secretagogue receptor (GHS-R1a), Ghrelin receptor, Anterior pituitary somatotrophs, Hypothalamic GHRH/somatostatin neurons
Metabolic healthSubcutaneousEvidence 5/5
Glucagon binds the hepatic glucagon receptor (GCGR), raising cyclic AMP to stimulate glycogenolysis and gluconeogenesis, which increases blood glucose as the body's main counter-regulatory hormone opposing insulin.
- Class
- Glucagon receptor (GCGR) agonist; counter-regulatory pancreatic hormone
- Dose ref
- Reference (label, not a recommendation): 1 mg SC/IM/IV injectable for severe hypoglycemia in adults; Gvoke 0.5 mg pediatric / 1 mg adult SC; Baqsimi 3 mg single intranasal dose; 0.25-2 mg IV/IM as a GI diagnostic aid
- Half-life
- Short; roughly 8-18 minutes for native glucagon (pharmacokinetic studies)
- Targets
- Glucagon receptor (GCGR)
Reproductive & hormoneImplantEvidence 5/5
Goserelin is a synthetic decapeptide GnRH agonist that first stimulates and then, with continuous depot exposure, downregulates pituitary GnRH receptors to suppress LH, FSH and downstream sex steroids toward castrate or postmenopausal levels.
- Class
- GnRH (LHRH) agonist decapeptide
- Dose ref
- Label reference (not a recommendation): 3.6 mg subcutaneous depot every 28 days, or 10.8 mg subcutaneous depot every 12 weeks for prostate cancer.
- Half-life
- Serum elimination half-life of the drug is about 4 hours with normal renal function (up to ~12 hours with severe renal impairment); the depot provides sustained release over 4 to 12 weeks
- Targets
- GnRH receptor, pituitary gonadotrophs, LH, FSH, testosterone, estradiol
Weight lossSubcutaneousEvidence 2/5
A synthetic C-terminal fragment of human growth hormone claimed to stimulate adipocyte lipolysis without binding the GH receptor or raising IGF-1, though human fat-loss evidence is weak.
- Class
- Growth hormone C-terminal lipolytic fragment
- Dose ref
- No established human dose; research-only
- Half-life
- Very short (minutes); poorly characterized
- Targets
- Adipocyte lipid metabolism
Reproductive & hormoneImplantEvidence 4/5
Histrelin is a GnRH receptor agonist that initially stimulates and then, through continuous implant delivery, downregulates pituitary GnRH receptors to suppress LH, FSH and sex steroid production.
- Class
- GnRH agonist (gonadotropin-releasing hormone agonist)
- Dose ref
- Reference (not a recommendation): one 50 mg subcutaneous implant per 12 months, delivering roughly 50-65 mcg histrelin per day per FDA labels.
- Half-life
- Continuous release for ~12 months from the implant; terminal half-life of the peptide is ~3.9 hours (clearance ~179 mL/min) after the implant is removed.
- Targets
- GnRH receptor, Pituitary gonadotrophs, LH/FSH secretion
LongevitySubcutaneousEvidence 2/5
Humanin is a 24-amino-acid mitochondrial-derived peptide that limits stress-induced apoptosis by binding pro-apoptotic proteins (BAX, Bid/Bim) and IGFBP-3 intracellularly and by signaling extracellularly through FPR2/FPRL1 and the CNTFR/WSX-1/gp130 complex to activate JAK2/STAT3, ERK1/2 and AKT survival pathways.
- Class
- Mitochondrial-derived peptide (cytoprotective/anti-apoptotic signaling peptide)
- Dose ref
- Research-only; no validated or approved human dose. Preclinical studies typically use the potent analog HNG (S14G-humanin) in animal models (e.g., microgram-to-milligram-per-kg, intermittent injection) - these are experimental figures, not human dosing recommendations.
- Half-life
- Not formally characterized in humans; native humanin is reported to clear rapidly, and engineered analogs such as HNG were developed for greater stability and potency.
- Targets
- FPR2/FPRL1, FPRL2, CNTFR/WSX-1/gp130 receptor complex, BAX, IGFBP-3
Growth hormoneSubcutaneousEvidence 2/5
Removal of the N-terminal tripeptide sharply lowers IGF-binding-protein affinity while preserving IGF-1 receptor binding, leaving more free peptide to activate IGF-1R.
- Class
- Truncated IGF-1 analog
- Dose ref
- No established human dose; research-only
- Half-life
- Very short; minutes in animal studies
- Targets
- IGF-1R
Growth hormoneSubcutaneousEvidence 2/5
A modified IGF-1 that binds IGF binding proteins far more weakly than native IGF-1, leaving it free to act as a potent, long-acting agonist at the IGF-1 receptor.
- Class
- IGF-1 analog / IGF-1 receptor agonist (research reagent)
- Dose ref
- No validated human dose; research reagent only
- Half-life
- ~20-30 hours (reported, non-clinical estimate)
- Targets
- IGF-1R
Growth hormoneSubcutaneousEvidence 3/5
Selectively stimulates pituitary growth hormone release without significant cortisol or prolactin elevation seen with older GHRPs.
- Class
- Selective GH secretagogue (GHRP)
- Dose ref
- 100–300 mcg per injection (research)
- Half-life
- ~2 hours
- Targets
- GHSR / ghrelin receptor
Somatuline Depot, Somatuline Autogel
ApprovedClinical / approved drugSubcutaneousEvidence 5/5
Lanreotide binds with high affinity to somatostatin receptors 2 and 5, mimicking native somatostatin to suppress growth hormone, IGF-1 and various neuroendocrine and gut hormones.
- Class
- Long-acting somatostatin analog (cyclic octapeptide)
- Dose ref
- Per FDA label (not a recommendation): acromegaly 60-120 mg deep subcutaneously every 4 weeks (typically starting at 90 mg); GEP-NET and carcinoid syndrome 120 mg every 4 weeks.
- Half-life
- Depot-dominated: apparent terminal elimination of about 23-30 days due to slow release from the subcutaneous gel depot
- Targets
- SSTR2, SSTR5
Larazotide acetate, AT-1001
InvestigationalClinical / approved drugOralEvidence 2/5
An oral, gut-restricted peptide that antagonizes zonulin signaling to limit gluten-driven intestinal tight-junction permeability in celiac disease.
- Class
- Tight-junction regulator / zonulin antagonist
- Dose ref
- Investigational; 0.5 mg orally three times daily in trials
- Half-life
- Minimal systemic absorption (gut-restricted)
- Targets
- Zonulin / tight junctions
Weight lossSubcutaneousEvidence 5/5
Daily GLP-1 analog. Reduces appetite and improves glycemic control via the same incretin pathway as semaglutide.
- Class
- GLP-1 receptor agonist
- Dose ref
- 0.6–3.0 mg once daily
- Half-life
- ~13 hours
- Targets
- GLP-1R
Weight lossSubcutaneousEvidence 4/5
Lixisenatide is an exendin-4-derived GLP-1 receptor agonist that slows gastric emptying and lowers postprandial glucose while stimulating glucose-dependent insulin release and suppressing glucagon.
- Class
- Short-acting (prandial) GLP-1 receptor agonist; exendin-4-derived peptide
- Dose ref
- Reference (Adlyxin label, not a recommendation): 10 mcg once daily subcutaneously for 14 days, then 20 mcg once daily maintenance, injected within one hour before the first meal.
- Half-life
- Approximately 3 hours (reported range ~2.7-4.3 hours)
- Targets
- GLP-1 receptor (GLP-1R)
Palmitoyl Pentapeptide-4, pal-KTTKS, Matrixyl 3000
Research onlySkin & cosmeticTopicalEvidence 2/5
A palmitoylated matrikine derived from the type I procollagen C-terminal propeptide that signals dermal fibroblasts to increase extracellular matrix synthesis, including type I and III collagen and fibronectin.
- Class
- Cosmetic matrikine peptide (collagen-stimulating)
- Dose ref
- No medical dose; pivotal cosmetic trials used pal-KTTKS at ~3 ppm (about 0.0003%) topically twice daily - a study condition, not a recommendation.
- Half-life
- Not characterized; a topical cosmetic ingredient with no established systemic pharmacokinetic half-life.
- Targets
- Dermal fibroblasts, Type I collagen, Type III collagen, Fibronectin, Extracellular matrix
Antimicrobial & immuneSubcutaneousEvidence 2/5
Melittin inserts into lipid bilayers and folds into an amphipathic alpha-helix that forms transmembrane toroidal pores, disrupting the membrane and lysing cells without binding a specific receptor.
- Class
- Cytolytic antimicrobial (membrane-active) peptide
- Dose ref
- No validated human dose; in vitro antibacterial MIC values reported around 8-32 ug/mL (laboratory measurements, explicitly not dosing recommendations)
- Half-life
- Not established in humans; reviews report rapid plasma degradation and poor pharmacokinetics
- Targets
- Phospholipid bilayer membranes, Microbial cell membranes, Cancer cell membranes
MGF (Mechano Growth Factor)
Growth hormoneSubcutaneousEvidence 2/5
MGF is the IGF-1Ec splice variant whose distinct C-terminal E-domain peptide, induced by mechanical loading or damage, is proposed to activate satellite cells ahead of mature IGF-1 signaling.
- Class
- IGF-1 splice variant / E-domain peptide
- Dose ref
- No established or approved human dose; research-only
- Half-life
- Very short; minutes for the native E-peptide
- Targets
- Satellite (muscle stem) cells, Myoblasts
CognitiveIntranasalEvidence 2/5
N-Acetyl Selank is a chemically stabilized (N-acetylated, C-amidated) analog of the tuftsin-derived peptide Selank, proposed to act via GABAergic modulation, inhibition of enkephalin-degrading enzymes that raises endogenous enkephalins, and BDNF-related effects, though these mechanisms were demonstrated for the parent Selank rather than the analog.
- Class
- Synthetic tuftsin-derived heptapeptide analog (anxiolytic neuropeptide)
- Dose ref
- No established human dose; research-only. Parent Selank was used intranasally in rodent studies at roughly 250-500 micrograms/kg, and Russian Selank nasal-drop clinical use is product-specific - neither is a validated guide for the acetylated analog and neither is a recommendation.
- Half-life
- Not validated for the analog. Parent Selank has a very short plasma half-life (on the order of minutes); N-terminal acetylation and C-terminal amidation are intended to slow enzymatic degradation, but no peer-reviewed human pharmacokinetic data exist for N-Acetyl Selank.
- Targets
- GABAergic system, Enkephalin-degrading enzymes (enkephalinase), BDNF expression, Serotonergic/monoaminergic systems
N-Acetyl Semax Amidate, NA Semax
Research onlyCognitiveIntranasalEvidence 2/5
It is a chemically stabilized analog of the ACTH(4-7)-derived peptide Semax that, in preclinical models, binds specifically in brain tissue and raises BDNF and other neurotrophins while modulating ischemia-related inflammatory and neurotransmitter gene expression.
- Class
- Synthetic ACTH(4-7)-derived melanocortin neuropeptide (acetylated/amidated Semax analog)
- Dose ref
- No established human dose for the N-acetylated/amidated analog; parent Semax was used intranasally at roughly 6,000-18,000 mcg/day in Russian stroke trials (research figures from trials, not recommendations)
- Half-life
- Not established for the analog; parent Semax plasma half-life is only minutes due to rapid aminopeptidase degradation, and vendor-claimed multi-hour half-lives lack peer-reviewed human PK data
- Targets
- BDNF/TrkB neurotrophin signaling, NGF/TrkA and NT-3/TrkC pathways, melanocortin (ACTH/MSH) system, dopaminergic and serotonergic neurotransmission
Reproductive & hormoneIntranasalEvidence 4/5
Nafarelin is a potent GnRH receptor agonist that initially stimulates pituitary LH and FSH release but with continued dosing downregulates the receptor, suppressing gonadotropins and sex steroid production.
- Class
- GnRH agonist (gonadotropin-releasing hormone analog)
- Dose ref
- Per the FDA label (reference only, not a recommendation): endometriosis 400 mcg/day (one 200 mcg spray per nostril twice daily), increasable to 800 mcg/day; central precocious puberty 1600 mcg/day, increasable to 1800 mcg/day.
- Half-life
- Approximately 3 hours in adults (about 2.5 hours in children) after intranasal administration
- Targets
- GnRH receptor (pituitary gonadotrophs), LH, FSH, estradiol, testosterone
Clinical / approved drugIntravenousEvidence 2/5
Nesiritide binds the particulate guanylate cyclase natriuretic peptide receptor on vascular smooth muscle and endothelial cells, raising intracellular cGMP to produce vasodilation and reduced cardiac filling pressures.
- Class
- Recombinant human B-type natriuretic peptide (vasodilator)
- Dose ref
- Label reference only (discontinued; NOT a recommendation): 2 mcg/kg IV bolus followed by a 0.01 mcg/kg/min continuous infusion
- Half-life
- ~18 minutes (terminal elimination; hemodynamic effects can persist several hours)
- Targets
- Natriuretic peptide receptor-A (NPR-A), Particulate (membrane-bound) guanylate cyclase
P021, CNTF-derived peptidergic compound
Research onlyCognitiveOralEvidence 2/5
P21 is a CNTF-derived peptide that increases BDNF expression, competitively inhibits leukemia inhibitory factor signaling, raises phosphorylated CREB and lowers GSK-3 beta activity to promote dentate gyrus neurogenesis and synaptic plasticity in animal models.
- Class
- CNTF-derived neurotrophic peptide mimetic
- Dose ref
- No established human dose; preclinical rodent studies used roughly 60 nmol/g of feed orally (about 162 nmol/mouse/day) - not a human recommendation.
- Half-life
- Not established in humans; preclinical reports describe plasma stability exceeding 3 hours and high gastric/intestinal stability.
- Targets
- CNTF signaling pathway, Leukemia inhibitory factor (LIF), BDNF/TrkB, CREB, GSK-3 beta
Clinical / approved drugSubcutaneousEvidence 4/5
Pasireotide is a multi-receptor somatostatin analog that binds somatostatin receptor subtypes 1, 2, 3 and 5 with high affinity for subtype 5, suppressing ACTH secretion in Cushing's disease and growth hormone and IGF-1 in acromegaly.
- Class
- Multi-receptor somatostatin analog (somatostatin receptor agonist)
- Dose ref
- Reference ranges (per labels, not recommendations): Signifor SC 0.3-0.9 mg twice daily for Cushing's disease; Signifor LAR 40 mg up to 60 mg intramuscular every 4 weeks for acromegaly
- Half-life
- Approximately 12-hour effective half-life for subcutaneous Signifor; Signifor LAR is a long-acting intramuscular depot
- Targets
- SSTR5, SSTR2, SSTR1, SSTR3
LongevityOralEvidence 2/5
Pinealon is proposed to penetrate cells and the blood-brain barrier and bind directly to DNA promoter regions and histone proteins, shifting expression of antioxidant and neuroprotective genes rather than acting through a classical membrane receptor.
- Class
- Synthetic short-peptide bioregulator (tripeptide)
- Dose ref
- No FDA-approved or validated human dose; research-only. Russian oral cytogen capsules and published study protocols describe past use, not dosing recommendations.
- Half-life
- Not formally characterized in humans; as an ultrashort peptide it is expected to clear from plasma rapidly (minutes).
- Targets
- DNA promoter regions / chromatin, Histone proteins, SOD2 (antioxidant gene), GPX1 (antioxidant gene), Neuronal apoptosis (caspase-3) pathways
Clinical / approved drugOralEvidence 4/5
Plecanatide is a uroguanylin analog that activates guanylate cyclase-C on the luminal surface of the intestine, raising cyclic GMP and driving chloride and bicarbonate secretion through CFTR to increase intestinal fluid and transit.
- Class
- Guanylate cyclase-C (GC-C) agonist
- Dose ref
- Reference (label, not a recommendation): one 3 mg tablet orally once daily; phase 3 trials studied 3 mg and 6 mg
- Half-life
- Not calculable; minimally absorbed with negligible systemic availability, plasma levels below limit of quantitation
- Targets
- Guanylate cyclase-C (GC-C), CFTR chloride channel, Intestinal epithelium
Weight lossSubcutaneousEvidence 4/5
Activates GLP-1, GIP and glucagon receptors simultaneously to suppress appetite and raise energy expenditure.
- Class
- Triple agonist (GLP-1 / GIP / glucagon)
- Dose ref
- 1–12 mg once weekly (trial)
- Half-life
- ~6 days
- Targets
- GLP-1R, GIPR, GCGR
ChiRhoStim, human secretin
ApprovedClinical / approved drugIntravenousEvidence 4/5
Secretin binds the secretin receptor on pancreatic duct cells, raising cAMP and opening CFTR channels to drive secretion of bicarbonate-rich pancreatic fluid that is measured during diagnostic testing.
- Class
- Gastrointestinal peptide hormone (diagnostic agent); secretin-receptor agonist
- Dose ref
- FDA label reference doses (diagnostic, not recommendations): 0.2 mcg/kg IV over 1 minute for pancreatic exocrine function testing or ERCP; 0.4 mcg/kg IV over 1 minute for gastrinoma testing.
- Half-life
- About 45 minutes per the ChiRhoStim label (synthetic human secretin); native secretin plasma half-life measured at roughly 4 minutes by radioimmunoassay.
- Targets
- Secretin receptor (SCTR), Pancreatic duct cells, CFTR channel, Gastrin secretion (G cells)
CognitiveIntranasalEvidence 3/5
Russian-developed analog of tuftsin marketed (in Russia) as an anxiolytic. Mechanism involves modulation of GABA and stress-response pathways.
- Class
- Synthetic tuftsin analog
- Dose ref
- 150–500 mcg per dose (intranasal, research)
- Half-life
- Minutes
- Targets
- GABAergic / serotonergic systems
Ozempic, Wegovy, Rybelsus
ApprovedWeight lossSubcutaneousEvidence 5/5
Mimics the incretin GLP-1, slowing gastric emptying and reducing appetite while improving insulin secretion.
- Class
- GLP-1 receptor agonist
- Dose ref
- 0.25–2.4 mg once weekly (SC); 3–14 mg daily (oral)
- Half-life
- ~7 days
- Targets
- GLP-1R
CognitiveIntranasalEvidence 2/5
Heptapeptide derived from ACTH(4-10). Russian neuropeptide studied for nootropic and neuroprotective effects, partly via BDNF upregulation.
- Class
- Synthetic ACTH analog
- Dose ref
- 200–600 mcg per dose (intranasal, research)
- Half-life
- Minutes
- Targets
- Melanocortin / BDNF pathways
Clinical / approved drugIntravenousEvidence 4/5
Sincalide is the synthetic C-terminal octapeptide of cholecystokinin that activates CCK receptors to stimulate gallbladder contraction, sphincter of Oddi relaxation and pancreatic secretion.
- Class
- Cholecystopancreatic-gastrointestinal hormone analog (diagnostic agent)
- Dose ref
- Reference diagnostic doses (not a recommendation): 0.02 mcg/kg IV over 30-60 seconds, or a 0.12 mcg/kg infusion over ~50-60 minutes; per the Kinevac label.
- Half-life
- Very short; serum half-life roughly 2.5 minutes per the label (volunteer studies near 1.3 minutes)
- Targets
- Cholecystokinin receptor (CCK-A / CCK1), Cholecystokinin receptor (CCK-B / gastrin)
Skin & cosmeticTopicalEvidence 2/5
SNAP-8 mimics the N-terminal of SNAP-25 and competes for its place in the SNARE complex, reducing the efficiency of neurotransmitter vesicle fusion and thereby modestly and reversibly lowering the muscle contraction that drives expression lines.
- Class
- Topical cosmetic neuromodulating peptide (SNAP-25 mimic)
- Dose ref
- Topical cosmetic use only; formulations commonly deliver roughly 3-10% of the supplier peptide blend (formulation reference levels, not clinical dosing recommendations).
- Half-life
- Not established for human use; a topical cosmetic ingredient with no defined systemic pharmacokinetic half-life.
- Targets
- SNAP-25, SNARE complex, neuromuscular junction acetylcholine release
Weight lossSubcutaneousEvidence 4/5
Co-activates GLP-1 and glucagon receptors; in Phase 2 produced substantial weight reduction and improvement in MASH endpoints.
- Class
- Dual agonist (GLP-1 / glucagon)
- Dose ref
- 0.6–4.8 mg once weekly (trial)
- Half-life
- ~7 days
- Targets
- GLP-1R, GCGR
Healing & recoverySubcutaneousEvidence 2/5
Synthetic fragment of thymosin β4 studied in animal models for cell migration, angiogenesis and tissue repair. No approved human indication.
- Class
- Thymosin β4 derivative
- Dose ref
- No human dosing established
- Half-life
- Not well characterized
- Targets
- G-actin
Forteo, Bonsity, PTH 1-34
ApprovedClinical / approved drugSubcutaneousEvidence 4/5
Once-daily injection produces intermittent activation of the PTH1 receptor on osteoblasts, preferentially stimulating bone formation over resorption to increase bone mass.
- Class
- Parathyroid hormone analog; anabolic (bone-forming) osteoporosis agent
- Dose ref
- 20 mcg subcutaneously once daily (labeled dose for Forteo and Bonsity; reference figure, not a recommendation)
- Half-life
- Approximately 1 hour after subcutaneous injection (a few minutes after IV); Forteo label
- Targets
- PTH1 receptor (PTH/PTHrP receptor), osteoblasts
Clinical / approved drugIntravenousEvidence 4/5
Terlipressin is a vasopressin V1 receptor agonist and prodrug for lysine-vasopressin that causes splanchnic vasoconstriction, lowering portal pressure and raising effective arterial volume and mean arterial pressure to improve renal perfusion.
- Class
- Synthetic vasopressin analog (V1 receptor agonist), prodrug of lysine-vasopressin
- Dose ref
- Reference label range (not a recommendation): Terlivaz 0.85 mg IV bolus every 6 hours (equal to 1 mg terlipressin acetate) for days 1-3, adjustable up to 1.7 mg every 6 hours, maximum 14 days
- Half-life
- Terlipressin terminal half-life about 0.9 hours; active metabolite lysine-vasopressin about 3.0 hours
- Targets
- Vasopressin V1A receptor, Vasopressin V1B/V3 receptor, Vasopressin V2 receptor (lower affinity)
Growth hormoneSubcutaneousEvidence 5/5
Stabilized GHRH analog. Approved for reduction of excess visceral abdominal fat in HIV-associated lipodystrophy.
- Class
- GHRH analog
- Dose ref
- 2 mg once daily
- Half-life
- ~26 minutes
- Targets
- GHRH receptor
thymus polypeptide fraction
Research onlyLongevityIntramuscularEvidence 2/5
Thymalin is a calf-thymus polypeptide complex proposed to act as an immunomodulator that promotes T-lymphocyte differentiation and maturation and normalizes cytokine and immune-cell balance, though its precise molecular receptor or target remains undefined.
- Class
- Thymic peptide bioregulator (immunomodulator / polypeptide extract)
- Dose ref
- Reference only, not a recommendation: Russian trials/labeling describe roughly 5-20 mg intramuscularly daily for short 5-10 day courses; the 2021 COVID-19 trial used 10 mg IM daily for 10 days.
- Half-life
- Not well characterized; short peptide complex with a presumed short plasma half-life (dosing relies on repeated daily courses).
- Targets
- T-lymphocyte differentiation and maturation, thymic and immune homeostasis, cytokine regulation (IL-2, interferon), hematopoietic stem cell differentiation
Glutamyl-Tryptophan, gamma-glutamyl-tryptophan
Research onlyLongevityIntramuscularEvidence 2/5
Thymogen is a synthetic L-glutamyl-L-tryptophan dipeptide that acts as a thymic-peptide immunomodulator, promoting T-lymphocyte differentiation and peptide-MHC recognition, shifting IL-2 and interferon cytokine output, and enhancing neutrophil chemotaxis and phagocytosis.
- Class
- Synthetic thymic-peptide immunomodulator (peptide bioregulator)
- Dose ref
- Russian product leaflet only (not a recommendation, not FDA-reviewed): ~100 mcg intramuscular once daily, roughly 300-1000 mcg per treatment course; intranasal spray ~25 mcg per metered dose. No validated dosing exists outside Russia.
- Half-life
- Not well characterized; as a small dipeptide it is expected to be rapidly hydrolyzed by serum and tissue peptidases (order of minutes). No reliable published human PK.
- Targets
- T-lymphocytes (differentiation, peptide-MHC recognition), Neutrophils (chemotaxis, phagocytosis), IL-2 and interferon cytokine signaling, Thymic / adaptive immune regulation
Healing & recoverySubcutaneousEvidence 3/5
Thymosin beta-4 sequesters monomeric G-actin to regulate the actin cytoskeleton, enabling cell migration, angiogenesis and tissue repair, with an anti-fibrotic Ac-SDKP fragment.
- Class
- Endogenous actin-sequestering peptide (beta-thymosin family)
- Dose ref
- No established therapeutic dose; phase 1 IV studies used 42-1260 mg
- Half-life
- Short, dose-dependent ~1-2 hours (IV)
- Targets
- G-actin
FTS, facteur thymique serique, zinc-thymulin
Research onlyLongevitySubcutaneousEvidence 2/5
Thymulin is a thymic nonapeptide that becomes biologically active only when bound to zinc, after which it promotes T-cell differentiation, modulates cytokines, and participates in two-way neuroendocrine signaling.
- Class
- Zinc-dependent thymic peptide hormone (immunomodulatory nonapeptide)
- Dose ref
- No established human dose; reference figures derive only from animal and gene-therapy models, not approved human labels (research-only, NOT a recommendation).
- Half-life
- Not established in humans; the native peptide is cleared rapidly from circulation, which motivated stabilized analogs and gene-therapy delivery approaches.
- Targets
- T-cell differentiation pathways, Thymic epithelial signaling, Neuroendocrine/pituitary axis, Cytokine regulation
LY3298176, Mounjaro, Zepbound
ApprovedWeight lossSubcutaneousEvidence 5/5
Activates GLP-1 and GIP receptors to improve glycemic control and reduce appetite + body weight.
- Class
- Dual agonist (GLP-1 / GIP)
- Dose ref
- 2.5–15 mg once weekly
- Half-life
- ~5 days
- Targets
- GLP-1R, GIPR
Reproductive & hormoneIntramuscularEvidence 5/5
Triptorelin is a potent GnRH-receptor agonist that first transiently stimulates LH and FSH release, then, with continuous exposure, downregulates and desensitizes pituitary GnRH receptors to suppress gonadotropins and sex steroids.
- Class
- GnRH agonist (synthetic decapeptide analog)
- Dose ref
- Label reference doses (not recommendations): Trelstar IM 3.75 mg every 4 weeks, 11.25 mg every 12 weeks, or 22.5 mg every 24 weeks; Triptodur IM 22.5 mg every 24 weeks for CPP.
- Half-life
- Terminal plasma half-life ~3 hours after IV dosing, but depot formulations release the peptide over 4 to 24 weeks.
- Targets
- Pituitary GnRH receptor (GnRHR)
LongevitySubcutaneousEvidence 2/5
Tuftsin, a tetrapeptide cleaved from the Fc region of IgG, binds the receptor neuropilin-1 and signals through the transforming growth factor beta pathway to stimulate phagocytosis and related innate immune cell functions.
- Class
- Immunomodulatory phagocytosis-stimulating tetrapeptide
- Dose ref
- No approved or established human dose; used at nanomolar concentrations in vitro and by injection in animal and small early-phase human research only (not a recommendation).
- Half-life
- Very short; the native tetrapeptide is rapidly degraded by aminopeptidases (minutes or less).
- Targets
- Neuropilin-1 (Nrp1), TGF-beta receptor-1, Macrophages, Neutrophils, Microglia
Clinical / approved drugIntravenousEvidence 4/5
Vasopressin activates V1a receptors on vascular smooth muscle to cause vasoconstriction and V2 receptors in the renal collecting duct to drive aquaporin-2-mediated water reabsorption, raising blood pressure and concentrating urine.
- Class
- Endogenous nonapeptide hormone; vasopressor / antidiuretic hormone
- Dose ref
- Label reference ranges (not recommendations): post-cardiotomy shock 0.03-0.1 units/min IV; septic shock 0.01-0.07 units/min IV continuous infusion
- Half-life
- Short; apparent half-life roughly 10 minutes or less per the Vasostrict label
- Targets
- V1a receptor, V2 receptor, V1b (V3) receptor
LongevitySubcutaneousEvidence 2/5
Vesugen (Lys-Glu-Asp) is proposed to enter the cell nucleus and bind DNA and histones in gene promoter regions, modulating expression of vascular, senescence and neurogenesis genes rather than acting as a classical receptor agonist.
- Class
- Short-peptide bioregulator (synthetic tripeptide)
- Dose ref
- No approved or established human dose; research-only. Figures cited for Russian supplement courses or reconstituted research vials are not dosing recommendations.
- Half-life
- No published human pharmacokinetic data; as an ultrashort tripeptide it is expected to clear from plasma within minutes.
- Targets
- Gene promoter regions / DNA, Histone proteins, Endothelin-1 expression, Connexins, Sirtuin-1 (SIRT1)
LongevityIntramuscularEvidence 2/5
Vilon is a synthetic Lys-Glu dipeptide proposed to enter cells, bind sequence-specific sites in gene-promoter DNA and remodel chromatin, thereby modulating expression of immune- and proliferation-related genes, an effect shown mainly in rodent and cell-culture models.
- Class
- Synthetic dipeptide bioregulator (research-only peptide immunomodulator/geroprotector)
- Dose ref
- No validated or approved human dose; Russian experimental/clinical work used short intramuscular injection courses and rodent studies used microgram-to-milligram parenteral doses (research only, not a recommendation)
- Half-life
- Not formally characterized in humans; as an ultra-short dipeptide, plasma half-life is expected to be very short (on the order of minutes)
- Targets
- Gene-promoter DNA / chromatin, Thymic epithelial cells and T-lymphocytes, Immune gene expression (e.g., IL-2)
VIP (Vasoactive Intestinal Peptide)
Healing & recoveryIntranasalEvidence 2/5
VIP activates VPAC1 and VPAC2 receptors, raising intracellular cyclic AMP to drive vasodilation, smooth-muscle relaxation and immune modulation.
- Class
- Neuropeptide; VPAC1/VPAC2 receptor agonist
- Dose ref
- Route-dependent (investigational); e.g. inhaled aviptadil 50 mcg four times daily in studies
- Half-life
- ~1 minute (plasma)
- Targets
- VPAC1, VPAC2
Prialt, SNX-111, omega-conotoxin MVIIA
ApprovedClinical / approved drugIntrathecalEvidence 4/5
Ziconotide binds and blocks N-type voltage-gated calcium channels on primary nociceptive afferents in the spinal dorsal horn, preventing presynaptic calcium influx and the release of pain-signaling neurotransmitters.
- Class
- Non-opioid N-type voltage-gated calcium channel blocker
- Dose ref
- Per the Prialt label (reference only, not a recommendation): initiate at no more than 2.4 mcg/day (0.1 mcg/hr) intrathecally, titrate up to 2.4 mcg/day at intervals no more than 2-3 times per week, to a recommended maximum of 19.2 mcg/day (0.8 mcg/hr) by about day 21.
- Half-life
- Serum half-life approximately 1.3 hours; cleared from CSF with a mean half-life of about 4.6 hours (per Prialt label).
- Targets
- N-type (Cav2.2) voltage-gated calcium channels, Dorsal horn primary nociceptive afferents (Rexed laminae I-II)