Bremelanotide

Summary

Bremelanotide (CHEMBL2070241) is an approved protein (ATC G02CX05) targeting MC1R, MC3R, and MC4R; indicated across 3 conditions including physiological sexual disorder and kidney disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: G02CX05
• Targets: 4 (MC1R, MC3R, MC4R…)
• Indications: 3 conditions
• Clinical trials: 9
• Chemistry: 1025.2 Da · C50H68N14O10

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2070241
Name	Bremelanotide
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	9941379
ATC	G02CX05
Molecular formula	C50H68N14O10
Molecular weight	1025.2
InChIKey	FFHBJDQSGDNCIV-MFVUMRCOSA-N

SMILES: CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)O)NC(=O)C

IUPAC name: (3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxylic acid

Also known as: Bremelanotida, Bremelanotide, PT-141, PT-141 FREE BASE, BREMELANOTIDE, BREMELANOTIDE (ACETATE), Bremelanotide (Acetate)

Parent form; salt/anhydrous children: CHEMBL4297533

Patent coverage: 60 distinct patent families (157 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 142 (90%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
MC1R	MC1 receptor	Agonist	8.19	1%	Q01726
MC3R	MC3 receptor	Agonist	7.28	0.1%	P41968
MC4R	MC4 receptor	Agonist	9.6	0%	P32245
MC5R	MC5 receptor	Agonist	7.77	0%	P33032

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Melanocortin receptor 4, Melanocyte-stimulating hormone receptor, Melanocortin receptor 5, Melanocortin receptor 3.

Bioactivity

ChEMBL activities: 28 potent at pChembl ≥ 5 of 28 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MC1R	10.11	EC50	0.08	nM	CHEMBL_ACT_24362736
MC1R	10.11	EC50	0.08	nM	CHEMBL_ACT_24697695
MC1R	10.02	EC50	0.1	nM	CHEMBL_ACT_18227700
MC4R	9.92	EC50	0.12	nM	CHEMBL_ACT_24362935
MC4R	9.7	EC50	0.2	nM	CHEMBL_ACT_10992093
MC4R	9.61	EC50	0.25	nM	CHEMBL_ACT_18227740
MC4R	9.6	Ki	0.25	nM	CHEMBL_ACT_10992074
MC3R	9.17	EC50	0.68	nM	CHEMBL_ACT_24362764
MC3R	9.17	EC50	0.68	nM	CHEMBL_ACT_24697729
MC4R	8.84	EC50	1.45	nM	CHEMBL_ACT_24362792
MC4R	8.84	EC50	1.45	nM	CHEMBL_ACT_24697760
MC1R	8.72	Ki	1.91	nM	CHEMBL_ACT_18227612
MC1R	8.72	Ki	1.91	nM	CHEMBL_ACT_24362820
MC1R	8.72	Ki	1.91	nM	CHEMBL_ACT_24697602
MC3R	8.62	EC50	2.4	nM	CHEMBL_ACT_18227719
MC4R	8.39	EC50	4.07	nM	CHEMBL_ACT_18227940
MC1R	8.19	Ki	6.4	nM	CHEMBL_ACT_10992017
MC5R	7.77	Ki	17	nM	CHEMBL_ACT_10992055
MC4R	7.7	Ki	19.95	nM	CHEMBL_ACT_24697664
MC4R	7.66	Ki	21.88	nM	CHEMBL_ACT_24362876
MC4R	7.61	Ki	24.55	nM	CHEMBL_ACT_18227651
MC3R	7.28	Ki	53	nM	CHEMBL_ACT_10992036
MC3R	6.72	Ki	190.6	nM	CHEMBL_ACT_18227903
MC5R	6.71	IC50	195	nM	CHEMBL_ACT_18227672
MC3R	6.7	Ki	199.5	nM	CHEMBL_ACT_24362848
MC5R	6.7	IC50	199.5	nM	CHEMBL_ACT_24362904
MC3R	6.7	Ki	199.5	nM	CHEMBL_ACT_24697633
MC5R	6.7	IC50	199.5	nM	CHEMBL_ACT_24697791

Target pathways

Aggregated over 4 target gene(s): MC1R, MC3R, MC4R, MC5R.

Top Reactome pathways

10 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	4	MC1R, MC3R, MC4R, MC5R
Signal Transduction	4	MC1R, MC3R, MC4R, MC5R
Signaling by GPCR	4	MC1R, MC3R, MC4R, MC5R
Class A/1 (Rhodopsin-like receptors)	4	MC1R, MC3R, MC4R, MC5R
Peptide ligand-binding receptors	4	MC1R, MC3R, MC4R, MC5R
GPCR downstream signalling	4	MC1R, MC3R, MC4R, MC5R
G alpha (s) signalling events	4	MC1R, MC3R, MC4R, MC5R
GPCR ligand binding	4	MC1R, MC3R, MC4R, MC5R
MITF-M-regulated melanocyte development	4	MC1R, MC3R, MC4R, MC5R
Transcriptional and post-translational regulation of MITF-M expression and activity	4	MC1R, MC3R, MC4R, MC5R

Dominant GO biological processes

GO term	Targets
adenylate cyclase-activating G protein-coupled receptor signaling pathway	4
signal transduction	4
G protein-coupled receptor signaling pathway	4
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	3
regulation of feeding behavior	3
phospholipase C-activating G protein-coupled receptor signaling pathway	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	2
UV protection	1
sensory perception of pain	1
negative regulation of tumor necrosis factor production	1
intracellular signal transduction	1
melanin biosynthetic process	1
pigmentation	1
positive regulation of transcription by RNA polymerase II	1
positive regulation of melanin biosynthetic process	1

Indications & clinical

Indications

2 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
physiological sexual disorder	3	MONDO:0002134	EFO:0004714
kidney disorder	2	MONDO:0005240	EFO:0003086

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE2	4
PHASE3	3
PHASE4	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04179734	PHASE4	COMPLETED	Role of the Melanocortin-4 Receptor in Hypoactive Sexual Desire Disorder
NCT02333071	PHASE3	COMPLETED	1. Study to Evaluate the Efficacy/Safety of Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder
NCT02338960	PHASE3	COMPLETED	2. Study to Evaluate the Efficacy/Safety of Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder
NCT04943068	PHASE3	COMPLETED	A Phase 3, Bridging, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate the Efficacy and Safety of Subcutaneously Administered Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder (With or Without Decreased Arousal)
NCT06565611	PHASE2	ACTIVE_NOT_RECRUITING	A Phase 2 Study Evaluating the Co-Administration of Bremelanotide With Tirzepatide for the Treatment of Obesity
NCT00425256	PHASE2	COMPLETED	Evaluate the Safety and Efficacy of Bremelanotide in Women With Female Sexual Arousal Disorder (FSAD)
NCT01382719	PHASE2	COMPLETED	Bremelanotide in Premenopausal Women With Female Sexual Arousal Disorder and/or Hypoactive Sexual Desire Disorder
NCT05709444	PHASE2	COMPLETED	A Phase IIb, Multicenter, Open-Label, Prospective Study of Bremelanotide in Diabetic Kidney Disease
NCT03973047	PHASE1	COMPLETED	Study to Evaluate Rate of Nausea in Healthy Premenopausal Female Subjects Treated With Single Dose of Bremelanotide Alone or With Zofran

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

173 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
AFAMELANOTIDE	ChEMBL + PubChem	Phase 4 (approved)	MC1R, MC3R, MC4R, MC5R
SETMELANOTIDE	ChEMBL + PubChem	Phase 4 (approved)	MC1R, MC3R, MC4R, MC5R
INTERMEDINE	ChEMBL	Phase 2	MC1R, MC3R, MC4R, MC5R
AMIODARONE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
COLISTIN	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
MICONAZOLE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
SERTRALINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
TAMOXIFEN	ChEMBL	Phase 4 (approved)	MC3R, MC4R, MC5R
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
Ivacaftor	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
Linagliptin	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
PYRAZINAMIDE	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	MC3R, MC4R
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
AMLODIPINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
ANTAZOLINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
BEPRIDIL	ChEMBL	Phase 4 (approved)	MC3R, MC4R
BOSUTINIB	ChEMBL	Phase 4 (approved)	MC3R, MC4R
CARVEDILOL	ChEMBL	Phase 4 (approved)	MC3R, MC4R
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
CLEMASTINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
DULOXETINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
ECONAZOLE	ChEMBL	Phase 4 (approved)	MC3R, MC5R
FENOTEROL	ChEMBL	Phase 4 (approved)	MC3R, MC4R
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
GRAMICIDIN	ChEMBL	Phase 4 (approved)	MC4R, MC5R
HALOPERIDOL	ChEMBL	Phase 4 (approved)	MC3R, MC4R
IMIPRAMINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
LIDOCAINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
MEFLOQUINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
MITOXANTRONE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
MODAFINIL	ChEMBL	Phase 4 (approved)	MC3R, MC4R
NAFARELIN	ChEMBL	Phase 4 (approved)	MC3R, MC4R
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
PROMETHAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
RIFAXIMIN	ChEMBL	Phase 4 (approved)	MC3R, MC4R
RIMONABANT	ChEMBL	Phase 4 (approved)	MC3R, MC4R
ROSIGLITAZONE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
TERFENADINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
THIORIDAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
TRIFLUOPERAZINE	ChEMBL	Phase 4 (approved)	MC3R, MC4R
PL-8177	ChEMBL	Phase 2	MC1R, MC4R
Abiraterone	PubChem	Approved	MC3R, MC4R
Aclidinium Bromide	PubChem	Approved	MC3R, MC4R
Acyclovir	PubChem	Approved	MC3R, MC4R
Allopurinol	PubChem	Approved	MC3R, MC4R
Alogliptin	PubChem	Approved	MC3R, MC4R
Amiloride	PubChem	Approved	MC3R, MC4R
Anagrelide	PubChem	Approved	MC3R, MC4R
Aprepitant	PubChem	Approved	MC3R, MC4R
Atazanavir	PubChem	Approved	MC3R, MC4R
Betamethasone Valerate	PubChem	Approved	MC3R, MC4R
Bosentan	PubChem	Approved	MC3R, MC4R
Clofarabine	PubChem	Approved	MC3R, MC4R
Dacarbazine	PubChem	Approved	MC3R, MC4R
Desoxycorticosterone Pivalate	PubChem	Approved	MC3R, MC4R
Didanosine	PubChem	Approved	MC3R, MC4R
Dihydroergotamine	PubChem	Approved	MC3R, MC4R
Docetaxel	PubChem	Approved	MC3R, MC4R
Erythromycin	PubChem	Approved	MC3R, MC4R
Ethambutol	PubChem	Approved	MC3R, MC4R
Fidaxomicin	PubChem	Approved	MC3R, MC4R
Glycopyrrolate	PubChem	Approved	MC3R, MC4R
Methotrexate	PubChem	Approved	MC3R, MC4R
Moxifloxacin	PubChem	Approved	MC3R, MC4R
Naproxen	PubChem	Approved	MC3R, MC4R
Olanzapine	PubChem	Approved	MC3R, MC4R
Olmesartan Medoxomil	PubChem	Approved	MC3R, MC4R
Pramipexole	PubChem	Approved	MC3R, MC4R
Propoxyphene	PubChem	Approved	MC3R, MC4R
rifampin	PubChem	Approved	MC3R, MC4R
Sildenafil	PubChem	Approved	MC3R, MC4R
Spectinomycin	PubChem	Approved	MC3R, MC4R
Sulindac	PubChem	Approved	MC3R, MC4R
Tadalafil	PubChem	Approved	MC3R, MC4R
Tamsulosin	PubChem	Approved	MC3R, MC4R
Tiotropium Bromide Monohydrate	PubChem	Approved	MC3R, MC4R
Valacyclovir	PubChem	Approved	MC3R, MC4R
Valganciclovir	PubChem	Approved	MC3R, MC4R
Vancomycin	PubChem	Approved	MC3R, MC4R
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	MC3R
CINACALCET	ChEMBL + PubChem	Phase 4 (approved)	MC3R
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	MC3R
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	MC3R
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	MC3R
CAFFEINE	ChEMBL	Phase 4 (approved)	MC3R
CANNABIDIOL	ChEMBL	Phase 4 (approved)	MC3R
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	MC3R
CISPLATIN	ChEMBL	Phase 4 (approved)	MC5R
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	MC4R
COSYNTROPIN	ChEMBL	Phase 4 (approved)	MC4R
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	MC3R
DESERPIDINE	ChEMBL	Phase 4 (approved)	MC4R