Bremelanotide

Bremelanotide
Clinical data
Pronunciation/ˌbrɛmɪˈlænətaɪd/ ⓘ
Trade namesVyleesi
Other namesPT-141; Rekynda, bremelanotide acetate (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa619054
License data
Routes of
administration		Subcutaneous[1]
Drug classMelanocortin receptor agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilitySCTooltip Subcutaneous injection: ~100%[1]
Protein binding21%[1]
MetabolismHydrolysis of peptide bonds[1]
Elimination half-life2.7 hours[1]
ExcretionUrine: 64.8%
Feces: 22.8%
Identifiers
IUPAC name
  • (3S,6S,9R,12S,15S,23S)-15-[(N-Acetyl-L-norleucyl)amino]-9-benzyl-6-{3-[(diaminomethylidene)amino]propyl}-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxylic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC50H68N14O10
Molar mass1025.182 g·mol−1
3D model (JSmol)
SMILES
  • O=C(C)N[C@@H](CCCC)C(N[C@@H]1C(N[C@@H](CC2=CNC=N2)C(N[C@H](CC3=CC=CC=C3)C(N[C@@H](CCC/N=C(N)\N)C(N[C@@H](CC4=CNC5C=CC=CC45)C(N[C@@H](CCCCNC(C1)=O)C(O)=O)=O)=O)=O)=O)=O)=O
InChI
  • InChI=1S/C50H68N14O10/c1-3-4-16-35(58-29(2)65)43(67)64-41-25-42(66)54-20-11-10-18-37(49(73)74)60-46(70)39(23-31-26-56-34-17-9-8-15-33(31)34)62-44(68)36(19-12-21-55-50(51)52)59-45(69)38(22-30-13-6-5-7-14-30)61-47(71)40(63-48(41)72)24-32-27-53-28-57-32/h5-9,13-15,17,26-28,35-41,56H,3-4,10-12,16,18-25H2,1-2H3,(H,53,57)(H,54,66)(H,58,65)(H,59,69)(H,60,70)(H,61,71)(H,62,68)(H,63,72)(H,64,67)(H,73,74)(H4,51,52,55)/t35-,36-,37-,38+,39-,40-,41-/m0/s1 Y
  • Key:FFHBJDQSGDNCIV-MFVUMRCOSA-N Y
  (verify)

Bremelanotide, sold under the brand name Vyleesi, is a medication used to treat low sexual desire in women.[2] Specifically it is used for low sexual desire which occurs before menopause and is not due to medical problems, psychiatric problems, or problems within the relationship.[3][4][2] It is given by an injection just under the skin of the thigh or abdomen.[2][4]

Common side effects include nausea, pain at the site of injection, and headache.[2] It may also cause a temporary increase in blood pressure and decrease in heart rate after each dose, and darkening of the gums, face, and breasts.[4] The medication is a peptide and acts by activating the melanocortin receptors.[1][5]

Bremelanotide was approved for medical use in the United States in 2019.[2][6] It was developed by Palatin Technologies.[7] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[8]

  1. ^ a b c d e f "Vyleesi- bremelanotide injection". DailyMed. 10 September 2019. Retrieved 20 November 2019.
  2. ^ a b c d e "Bremelanotide Acetate Monograph for Professionals". Drugs.com. Retrieved 24 October 2019.
  3. ^ Cite error: The named reference FDA2019 was invoked but never defined (see the help page).
  4. ^ a b c "Drug Trials Snapshots: Vyleesi". U.S. Food and Drug Administration (FDA). 12 July 2019. Archived from the original on 20 November 2019. Retrieved 20 November 2019. This article incorporates text from this source, which is in the public domain.
  5. ^ Kingsberg SA, Clayton AH, Pfaus JG (November 2015). "The Female Sexual Response: Current Models, Neurobiological Underpinnings and Agents Currently Approved or Under Investigation for the Treatment of Hypoactive Sexual Desire Disorder". CNS Drugs. 29 (11): 915–933. doi:10.1007/s40263-015-0288-1. PMID 26519340. S2CID 7437096.
  6. ^ "Drug Approval Package: Vyleesi". U.S. Food and Drug Administration (FDA). Archived from the original on 20 November 2019.
  7. ^ "Bremelanotide". AdisInsight. Retrieved 6 April 2017.
  8. ^ "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration. 31 December 2019. Archived from the original on 2 May 2020. Retrieved 15 September 2020.
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