Peringatan Keamanan

Currently there are no reports of overdoses of bremelanotide.^L9635 Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure.^L9635 In the event of an overdose, supportive measures should be used to address the associated symptoms.^L9635

Bremelanotide

DB11653

biotech approved investigational

Deskripsi

Bremelanotide is a 7 amino acid peptide used to treat hypoactive sexual desire disorder in premenopausal women.^L9635 Bremelanotide does not interact with alcohol.^A179686 The mechanism by which bremelanotide's action on receptors translates to a clinical effect is still unknown.^L9635

Bremelanotide was first described in the literature in 2003 when it was known by the investigational code PT-141.^A179683 Since then it was investigated for its place in treating sexual dysfunction in men and women but is now only indicated for women.A179683,A179686,L9635 Other drugs used to treat female sexual dysfunction include flibanserin, estrogen, ospemifene, and prasterone.^A179689

Bremelanotide was granted FDA approval on 21 June 2019.^L9635

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).[L9635]

Volume Distribusi The mean volume of distribution of bremelanotide is 25.0±5.8L.[L9635]

Klirens (Clearance) The mean clearance of bremelanotide is 6.5±1.0L/hr.[L9635]

Absorpsi

Bremelanotide has a T_max or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable.^L9635 The C_max is 72.8ng/mL and the AUC is 276hr\*ng/mL.^L9635

Metabolisme

Bremelanotide is a 7 amino acid and so its metabolism consists of multiple hydrolysis reactions.^L9635

Rute Eliminasi

64.8% of a radiolabelled dose is excreted in the urine and 22.8% of the dose is recovered in the feces.^L9635

Interaksi Obat

1 Data

Naltrexone

The serum concentration of Naltrexone can be decreased when it is combined with Bremelanotide.

Target Protein

Melanocyte-stimulating hormone receptor MC1R

Melanocortin receptor 4 MC4R

Melanocortin receptor 3 MC3R

Melanocortin receptor 5 MC5R

Adrenocorticotropic hormone receptor MC2R

Referensi & Sumber

Artikel (PubMed)

PMID: 12851303
Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY: PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102. doi: 10.1111/j.1749-6632.2003.tb03167.x.
PMID: 28189361
Clayton AH, Lucas J, DeRogatis LR, Jordan R: Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants. Clin Ther. 2017 Mar;39(3):514-526.e14. doi: 10.1016/j.clinthera.2017.01.018. Epub 2017 Feb 9.
PMID: 30251897
Miller MK, Smith JR, Norman JJ, Clayton AH: Expert opinion on existing and developing drugs to treat female sexual dysfunction. Expert Opin Emerg Drugs. 2018 Sep;23(3):223-230. doi: 10.1080/14728214.2018.1527901. Epub 2018 Oct 11.
PMID: 29225554
Both S: Recent Developments in Psychopharmaceutical Approaches to Treating Female Sexual Interest and Arousal Disorder. Curr Sex Health Rep. 2017;9(4):192-199. doi: 10.1007/s11930-017-0124-3. Epub 2017 Oct 19.

Link

FDA Approved Drug Products: Bremelanotide Injection

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

Vyleesi

Injection • 1.75 mg/0.3mL • Subcutaneous • US • Approved
Vyleesi

Injection • 1.75 mg/0.3mL • Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.