Bremelanotide
Bremelanotide API
Bremelanotideke ntho ea maiketsetsomelanocortin receptor agonistntshetswa pele bakeng sa kalafo yabothata ba takatso e matla ea thobalano (HSDD) in basali ba premenopausal. Joalo ka kalafo ea pele ea mantlha e lumelletsoeng ka kotloloho bakeng sa HSDD, Bremelanotide e emetse tsoelo-pele e kholo bophelong ba basali ba thobalano.
E amohetsoe ke US FDA ka 2019 tlasa lebitso la lebitsoVyleesi, Bremelanotide e fana ka tharollo e hlokahalang, e seng ea li-hormone bakeng sa basali ba nang le ho hloka takatso e tsitsitseng ea thobalano, e ke keng ea hlalosoa ka litaba tsa bongaka, tsa kelello, kapa tsa likamano.
Tsa ronaBremelanotide APIe hlahisoa ka "solid-phase peptide synthesis" (SPPS), ho netefatsa bohloeki bo phahameng, litšila tse tlase, le ho tsitsa ho loketseng bakeng sa liente tsa bongaka le tsa khoebo.
Mokhoa oa Ts'ebetso
Bremelanotide e sebetsa kaho kenya tšebetsong melanocortin receptors, haholo-holoMC4R (melanocortin-4 receptor)hotsamaiso ea methapo e bohareng. Ts'ebetso ena ho lumeloa hore e fetola litsela tsa hohypothalamustse amehang takatsong ea ho kopanela liphate.
Liphello tsa bohlokoa li kenyelletsa:
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E ntlafalitsoepontšo ea dopaminergic, ho khothalletsa thahasello ea thobalano
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Khatello ea litsela tsa inhibitory tse amang libido
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Ho feto-fetoha ha tsamaiso ea methapo e boharengntle le ho itšetleha ka lihomone tsa thobalano (e seng estrogenic, non-testosterone)
Mochine ona o etsa hore Bremelanotide e fapane le litlhare tsa setso tsa li-hormone 'me e loketse palo e pharaletseng ea basali.
Lipatlisiso tsa Tleliniki le Liphetho
Bremelanotide e hlahlobiloe ka makhetlo a mangataLiteko tsa bongaka tsa Phase 2 le Phase 3, e akarelletsang basali ba likete ba fumanoeng ba e-na le HSDD.
Liphuputso tsa bohlokoa li kenyelletsa:
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Ntlafatso ea bohlokoa ka lipaloho lintlha tsa takatso ea thobalano (e lekantsoeng ke FSFI-d)
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Phokotso ea matšoenyeho a amanang le takatso e tlase ea thobalano (e lekantsoeng ke FSDS-DAO)
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Ho qala ketso ka potlako(ka hare ho lihora), lumellatšebeliso e batloang pele ho thobalano
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E bonts'a katleho ho basalie nang le maemo a mahlahahlaha le ntle le yona(mohlala, khatello ea maikutlo, matšoenyeho)
Lithutong tsa bongaka, ho fihlela ho25%–35%ea bakuli ba bile le ntlafatso e utloahalang khahlano le placebo.
Tšireletseho le Mamello
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Litla-morao tse tloaelehileng li kenyelletsaho nyekeloa ke pelo, ho phopholetsa, lehlooho e opang- ka kakaretso e bonolo ebile e ikemela.
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Ho fapana le mahlahana a pele a melanocortin, Bremelanotide e joaloe sa amaneng le keketseho e kholo ea khatello ea mali kapa lebelo la peloho bakuli ba bangata.
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Joalo ka kalafo e batloang feela, e qoba ho pepesehela lihomone tse sa foleng mme e ka sebelisoa habonolo.
Tlhahiso le Boleng
Tsa ronaBremelanotide API:
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E entsoe ka ho sebelisa SPPS e tsoetseng pele ka katleho e phahameng
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E kopana le maemo a thata a machaba abohloeki, boitsebiso, le metsoako e setseng
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E loketse ho etsoa ka ente (joalo ka lipene tsa autoinjector tse tlatsitsoeng pele)
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E fumaneha kalihlopha tsa lifofane le tsa khoebo, e tšehetsang ka bobeli R&D le phepelo ea 'maraka
Matla a Phekolo
Ka ntle ho HSDD, mochine oa Bremelanotide o hlahisitse thahasello libakeng tse ling tsathobalano le neuroendocrine modulation, ho kenyelletsa:
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Ho se sebetse hantle ha banna ka thobalano
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Mathata a amanang le maikutlo
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Takatso ea lijo le taolo ea matla (ka melanocortin system)
Boemo ba eona ba peptide bo nang le litšobotsi tse ntle le ts'ebetso ea methapo e bohareng e tsoela pele ho ts'ehetsa nts'etsopele e ka bang teng libakeng tse haufi tsa kalafo.
