I-Bremelanotide

I-Bremelanotide API

I-BremelanotideiwukwenziwaI-melanocortin receptor agonisteyenzelwe ukwelashwa kwei-hypoactive sex desire disorder (HSDD) in abesifazane be-premenopausal. Njengokwelashwa kokuqala okusebenzayo okugunyazwe ngokukhethekile i-HSDD, i-Bremelanotide imele intuthuko enkulu empilweni yobulili yabesifazane.

Kugunyazwe yi-US FDA ngo-2019 ngaphansi kwegama lomkhiqizoVyleesi, I-Bremelanotide inikeza isixazululo esidingeka kakhulu, esingelona ama-hormone kwabesifazane ababhekene nokuntula isifiso socansi okuphikelelayo, esingenakuchazwa ngezinkinga zezokwelapha, ezingokwengqondo, noma zobudlelwane.

EyethuI-Bremelanotide APIikhiqizwa ngokusebenzisa i-solid-phase peptide synthesis (SPPS), iqinisekisa ukuhlanzeka okuphezulu, ukungcola okuphansi, kanye nokuvumelana okulungele imijovo yomtholampilo neyezohwebo.

Indlela Yokwenza

I-Bremelanotide isebenza ngeivuselela ama-melanocortin receptors, ikakhulukaziI-MC4R (i-melanocortin-4 receptor)kweisimiso sezinzwa esiphakathi. Lokhu kuvula kukholelwa ukuthi kuguqula izindlela ku-i-hypothalamusezihilelekile ekuvukeni nasekufisweni kobulili.

Imithelela ebalulekile ihlanganisa:

• Kuthuthukisiweisibonakaliso se-dopaminergic, ukukhuthaza isithakazelo socansi

• Ukucindezelwa kwezindlela zokuvimbela ezithinta i-libido

• Ukuguqulwa kwesistimu yezinzwa ephakathingaphandle kokuthembela kumahomoni ocansi (non-estrogenic, non-testosterone)

Lo mshini wenza i-Bremelanotide ihluke ekwelashweni kwamahomoni endabuko futhi ifanele abantu besifazane abaningi.

Ucwaningo Lwezempilo Nemiphumela

I-Bremelanotide ihlolwe ngokuphindaphindiweIsigaba sesi-2 nesigaba sesi-3 sokuhlolwa komtholampilo, okubandakanya izinkulungwane zabesifazane abatholakala bene-HSDD.

Okutholakele okubalulekile kuhlanganisa:

• Ukuthuthukiswa okuphawulekayo ngokwezibalokumaphuzu esifiso socansi (akalwa yi-FSFI-d)

• Ukunciphisa ukucindezeleka okuhlobene nesifiso esiphansi socansi (kukalwa yi-FSDS-DAO)

• Ukuqala kwesenzo esisheshayo(kungakapheli amahora), ukuvumelaukusetshenziswa okudingekayo ngaphambi kokwenza ucansi

• Kuboniswe ukusebenza ngempumelelo kwabesifazanenezimo ezihambisanayo nezingenayo(isb, ukudangala, ukukhathazeka)

Ezifundweni zomtholampilo, kuze kufike25%–35%yeziguli bathole ukuthuthuka okunengqondo uma kuqhathaniswa ne-placebo.

Ukuphepha Nokubekezeleleka

• Imiphumela emibi kakhulu ihlanganisaisicanucanu, ukushaywa umoya, futhiikhanda elibuhlungu- ngokuvamile imnene futhi iyazibekela imingcele.

• Ngokungafani nama-melanocortin angaphambilini, i-Bremelanotide injalookungahlotshaniswa nokwenyuka okuphawulekayo komfutho wegazi noma izinga lokushaya kwenhliziyoezigulini eziningi.

• Njengokwelashwa okudingeka kakhulu, kugwema ukuchayeka kwehomoni okungapheli futhi kungasetshenziswa ngokuguquguquka.

Ukukhiqiza kanye Nekhwalithi

EyethuI-Bremelanotide API:

• Ihlanganiswa kusetshenziswa i-SPPS ethuthukisiwe esebenza kahle kakhulu

• Ihlangabezana nezindinganiso zamazwe ngamazwe eziqinile zeubumsulwa, ubuwena, nezincibilikisi eziyinsalela

• Ilungele ukwakhiwa komjovo (njengamapeni e-autoinjector agcwaliswe ngaphambili)

• Itholakala kuamaqoqo okuhlola kanye nezikali zezentengiselwano, esekela kokubili i-R&D kanye nokuhlinzekwa kwemakethe

Amandla Okwelapha

Ngaphandle kwe-HSDD, indlela ye-Bremelanotide ibangele isithakazelo kwezinye izindawo zeubulili kanye neuroendocrine modulation, okuhlanganisa:

• Ukungasebenzi kahle kocansi kwabesilisa

• Izifo ezihlobene nemizwa

• Ukulawulwa kokudla kanye namandla (ngesistimu ye-melanocortin)

Iphrofayili yayo ye-peptide enesimo esihle kanye nomsebenzi wezinzwa ophakathi kuyaqhubeka nokusekela ukuthuthukiswa okungenzeka ezindaweni eziseduze zokwelapha.