Tesamorelin
Tesamorelin API
Tesamorelin ni imiti ya peptide ikora, izina ryuzuye ni ThGRF (1-44) NH₂, ni imisemburo ikura irekura imisemburo (GHRH). Itera pitoito y'imbere gusohora imisemburo ikura (GH) mu kwigana ibikorwa bya GHRH endogenous, bityo ikongera mu buryo butaziguye urwego rw'imikurire ya insuline imeze nka 1 (IGF-1), ikazana inyungu nyinshi muri metabolism no gusana ingirangingo.
Kugeza ubu, Tesamorelin yemerewe na FDA kuvura lipodystrofiya iterwa na virusi itera sida, cyane cyane mu kugabanya ibinure byo mu nda byo mu nda (visceral adipose tissue, VAT). Yakozweho kandi ubushakashatsi kuri ** kurwanya-gusaza, syndrome de metabolike, indwara yumwijima idafite inzoga (NAFLD / NASH) ** nizindi nzego, byerekana ibyifuzo byinshi.
Uburyo bwibikorwa
Tesamorelin ni peptide ya 44-amino acide ifite imiterere isa cyane na GHRH karemano. Uburyo bwibikorwa ni:
Koresha GHRH reseptor (GHRHR) kugirango ushishikarize pitoito imbere kurekura GH.
GH imaze kuzamurwa, ikora ku mwijima no mu ngingo ziyikikije kugirango yongere synthesis ya IGF-1.
GH na IGF-1 bafatanya muguhindura ibinure, synthesis ya protein, gusana ingirabuzimafatizo no kubungabunga amagufwa.
Ikora cyane cyane kubora ibinure byumubiri (mobilisation yibinure) kandi ntigira ingaruka nke kumavuta yo munsi.
Ugereranije no guterwa mu buryo butaziguye GH, Tesamorelin iteza imbere GH ikoresheje uburyo bwa endogenous, bwegereye injyana ya physiologique kandi ikirinda ingaruka mbi ziterwa na GH ikabije, nko gufata amazi no kurwanya insuline.
Ubushakashatsi nubuvuzi bwiza
Imikorere ya Tesamorelin yagenzuwe binyuze mu bigeragezo byinshi by’amavuriro, cyane cyane mu bice bikurikira:
1. Lipodystrofiya iterwa na virusi itera SIDA (ibimenyetso byemewe na FDA)
Tesamorelin irashobora kugabanya cyane TVA yo munda (ikigereranyo cyo kugabanuka kwa 15-20%);
Ongera urwego rwa IGF-1 kandi utezimbere imiterere yumubiri;
Kunoza imiterere yumubiri no kugabanya umutwaro wa psychologiya ujyanye no kugabana ibinure;
Ntabwo bigira ingaruka zikomeye kubinure byamavuta, ubwinshi bwamagufwa cyangwa imitsi.
2. Non-alcool steatohepatitis (NASH) na fibrosis yumwijima
Igeragezwa rya Clinical ryerekanye ko Tesamorelin ishobora kugabanya ibinure byumwijima (amashusho ya MRI-PDFF);
Byitezwe kunoza hepatocyte insuline;
Ifite akamaro kanini kubarwayi banduye virusi itera sida na NAFLD, kandi ifite uburyo bwo kurinda metabolike yagutse.
3. Indwara ya metabolike no kurwanya insuline
Tesamorelin igabanya cyane urugero rwa triglyceride n'umubyibuho ukabije wo munda;
Kunoza indangagaciro ya HOMA-IR kandi ifasha mukurwanya insuline;
Ubushakashatsi bwerekanye ko bushobora kongera intungamubiri za poroteyine zo mu mitsi, zifasha abakuze cyangwa indwara zidakira.
Umusaruro wa API no kugenzura ubuziranenge
Tesamorelin API itangwa nitsinda ryacu rya Gentolex ikoresha tekinoroji igezweho ya peptide synthesis (SPPS) kandi ikorerwa mubidukikije bya GMP. Ifite ibintu bikurikira:
Isuku ≥99% (HPLC)
Nta endotoxine, ibyuma biremereye, ibisigara bisigaye byujuje ibyangombwa
Urutonde rwa aside amine hamwe no kwemeza imiterere na LC-MS / NMR
Tanga garama-urwego kuri kilo-urwego rwabigenewe
