Bremelanotideis a syntheticmelanocortin receptor agonistyakagadziridzwa kurapwa kwehypoactive sex chido disorder (HSDD) in vakadzi vane premenopausal. Seyekutanga yepakati pekurapa kurapa yakanyatso kutenderwa HSDD, Bremelanotide inomiririra kufambira mberi kwakakosha muhutano hwepabonde hwevakadzi.
Yakatenderwa neUS FDA muna 2019 pasi pezita rechiratidzoVyleesi, Bremelanotide inopa pane-inoda, isiri-homoni mhinduro yevakadzi vanoramba vachishaya chido chepabonde, izvo zvisingagoni kutsanangurwa nemishonga, pfungwa, kana hukama nyaya.
YeduBremelanotide APIinogadzirwa kuburikidza ne-soli-phase peptide synthesis (SPPS), ichivimbisa kuchena kwepamusoro, kusvibiswa kwakaderera, uye kusimba kwakakodzera kukiriniki uye yekutengeserana injectable formulations.
Bremelanotide inoshanda neactivating melanocortin receptors, kunyanyaMC4R (melanocortin-4 receptor)mucentral nervous system. Iyi activation inofungidzirwa kuti inogadzirisa nzira muhypothalamusizvo zvinobatanidzwa mukukwezva pabonde uye chido.
Mhedzisiro yakakosha inosanganisira:
Enhanceddopaminergic chiratidzo, kukurudzira kufarira zvepabonde
Kudzvinyirirwa kweinhibitory nzira dzinokanganisa libido
Central nervous system modulationpasina kuvimba nehomoni dzepabonde (kwete-estrogenic, kwete-testosterone)
Iyi nzira inoita kuti Bremelanotide ive mutsauko kubva kune echinyakare mahomoni marapirwo uye akakodzera huwandu hwakawanda hwevakadzi.
Bremelanotide yakaongororwa mune dzakawandaPhase 2 uye Phase 3 kiriniki miedzo, zvinosanganisira zviuru zvevakadzi vakaonekwa vaine HSDD.
Zviwanikwa zvakakosha zvinosanganisira:
Statistically yakakosha kuvandudzikamune zvebonde zvibodzwa (zvinoyerwa neFSFI-d)
Kuderedza kushushikana kwakabatana nechishuwo chakaderera chepabonde (kuyerwa neFSDS-DAO)
Kurumidza kutanga kwechiito(mumaawa mashoma), kubvumirapa-kuda kushandiswa kusati kwaita zvepabonde
Yakaratidza kushanda kwevakadzine uye pasina comorbid mamiriro(semuenzaniso, kuora mwoyo, kuzvidya mwoyo)
Muzvidzidzo zvekiriniki, kusvika25%–35%yevarwere vakawana kuvandudzwa kunobatsira maringe ne placebo.
Migumisiro yakajairika inosanganisirakuda kurutsa, flushing,uyemusoro- kazhinji zvinyoro uye kuzviganhurira.
Kusiyana nekare melanocortin vamiririri, Bremelanotide iriisingabatanidzi nekuwedzera kukuru kweropa kana kurova kwemoyomuvarwere vakawanda.
Sekurapa-kwekuda kurapwa, inodzivirira kusingaperi mahormone kuratidzwa uye inogona kushandiswa zviri nyore.
YeduBremelanotide API:
Inogadzirwa uchishandisa advanced SPPS ine hunyanzvi hwepamusoro
Inosangana nezvimiro zvepasi rose zvekuchena, kuzivikanwa, uye zvakasara zvinonyungudutsa
Inokodzera kugadzirwa kwejekiseni (senge prefilled autoinjector pens)
Inowanikwa mupilot uye zvekutengesa-scale batches, inotsigira zvese R&D uye musika wekupa
Beyond HSDD, Bremelanotide's mechanism yakakurudzira kufarira kune dzimwe nzvimbo dzezvepabonde uye neuroendocrine modulation, kusanganisira:
Kusashanda zvakanaka kwemurume
Zvinetso zvine chekuita nemafungiro
Kudya uye simba regulation (kuburikidza nemelanocortin system)
Yayo inonyatso hunhu peptide mbiri uye yepakati tsinga chiitiko inoenderera ichitsigira inogona kusimudzira munzvimbo dziri pedyo dzekurapa.