bremelanotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| melanocortin receptor agonists; peptides and glycopeptides | 5329 | 189691-06-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. The mechanism by which VYLEESI improves HSDD in women is unknown. The MC1R is expressed on melanocytes; binding at this receptor leads to melanin expression and increased pigmentation
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 21, 2019 | FDA | AMAG PHARMS INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G02CX05 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Other gynecologicals |
| FDA EPC | N0000194029 | Melanocortin Receptor Agonist |
| FDA MoA | N0000194030 | Melanocortin Receptor Agonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Lack or loss of sexual desire | indication | 270903007 | DOID:13868 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.28 | acidic |
| pKa2 | 12.41 | acidic |
| pKa3 | 12.76 | acidic |
| pKa4 | 13.11 | acidic |
| pKa5 | 13.39 | acidic |
| pKa6 | 13.66 | acidic |
| pKa7 | 8.36 | Basic |
| pKa8 | 7.73 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | PALATIN TECHNOLOGIES | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 10286034 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | PALATIN TECHNOLOGIES | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 9352013 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | PALATIN TECHNOLOGIES | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 9700592 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | PALATIN TECHNOLOGIES | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 11590209 | April 29, 2041 | TREATING ACQUIRED, GENERALIZED HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) IN A PREMENOPAUSAL FEMALE PATIENT WITH CONTROLLED HYPERTENSION BY INJECTING BREMELANOTIDE MORE THAN ONCE WITH AT LEAST 24 HOURS BETWEEN DOSES AND NO MORE THAN 8 DOSES PER MONTH |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | PALATIN TECHNOLOGIES | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | June 21, 2024 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Melanocortin receptor 4 | GPCR | AGONIST | Kd | 8 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Melanocortin receptor 5 | GPCR | AGONIST | Ki | 7.77 | CHEMBL | ||||
| Melanocortin receptor 3 | GPCR | AGONIST | EC50 | 8.62 | CHEMBL | ||||
| Melanocyte-stimulating hormone receptor | GPCR | AGONIST | EC50 | 10.02 | CHEMBL | ||||
| Adrenocorticotropic hormone receptor | GPCR | AGONIST | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 6Y24O4F92S | UNII |
| 1607799-13-2 | SECONDARY_CAS_RN |
| C1721339 | UMLSCUI |
| CHEMBL2070241 | ChEMBL_ID |
| 9941379 | PUBCHEM_CID |
| DB11653 | DRUGBANK_ID |
| CHEMBL4297533 | ChEMBL_ID |
| D06569 | KEGG_DRUG |
| 8737 | INN_ID |
| 10408 | IUPHAR_LIGAND_ID |
| 018059 | NDDF |
| 018060 | NDDF |
| 427418003 | SNOMEDCT_US |
| 788500001 | SNOMEDCT_US |
| 4038620 | VANDF |
| 2176311 | RXNORM |
| 319387 | MMSL |
| 37138 | MMSL |
| d09322 | MMSL |
| C476721 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Vyleesi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64011-701 | INJECTION | 1.75 mg | SUBCUTANEOUS | NDA | 28 sections |
| Vyleesi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 80064-141 | INJECTION | 1.75 mg | SUBCUTANEOUS | NDA | 27 sections |
| Vyleesi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 80064-141 | INJECTION | 1.75 mg | SUBCUTANEOUS | NDA | 27 sections |