Tesamorelin
Tesamorelin API
Tesamorelin is a synthetic peptide drug, zita rakazara ndiThGRF (1-44) NH₂, iyo inokura hormone inoburitsa hormone (GHRH) analog. Iyo inokurudzira anterior pituitary kuti ibudise kukura kwehomoni (GH) nekufananidza chiito cheGHRH isingagumi, nokudaro nenzira isina kunanga kuwedzera kwehuwandu hwe insulini-kufanana nekukura chinhu 1 (IGF-1), kuunza mutsara wezvibatsiro mumasabolism uye kugadziriswa kwetishu.
Parizvino, Tesamorelin yakatenderwa neFDA kurapwa kweHIV-inoenderana ne lipodystrophy, kunyanya kudzikisa abdominal visceral mafuta accumulation (visceral adipose tissue, VAT). Yakave yakadzidzwawo zvakanyanya kune ** anti-kuchembera, metabolic syndrome, isiri-doro fatty chiropa chirwere (NAFLD/NASH) ** uye mamwe minda, ichiratidza yakafara tarisiro yekushandisa.
Nzira yekuita
Tesamorelin is 44-amino acid peptide ine chimiro chakafanana neGHRH yechisikigo. Iyo nzira yekuita kwayo ndeye:
Activate GHRH receptor (GHRHR) kuti ikurudzire anterior pituitary kuburitsa GH.
Mushure mokunge GH yakasimudzwa, inoshanda pachiropa uye matishu akakomberedza kuwedzera IGF-1 synthesis.
GH uye IGF-1 pamwe chete kutora chikamu mumafuta metabolism, protein synthesis, kugadzirwa kwesero uye kugadzirisa kwepfupa density.
Inonyanya kushanda pamafuta e-visceral mafuta (kuunganidza mafuta) uye ine zvishoma zvishoma pane subcutaneous mafuta.
Inofananidzwa nejekiseni yakananga yakananga yeGH, Tesamorelin inokurudzira GH secretion kuburikidza nemagetsi ekupedzisira, iyo iri pedyo neyo physiological rhythm uye inodzivirira maitiro akaipa anokonzerwa neGH yakawandisa, zvakadai sekuchengetedza mvura uye insulin kudzivisa.
Tsvakurudzo uye kushanda kwekiriniki
Kubudirira kweTesamorelin kwakave kwakasimbiswa kuburikidza neakawanda makiriniki miedzo, kunyanya munzvimbo dzinotevera:
1. HIV-inoenderana ne lipodystrophy (FDA-approved zviratidzo)
Tesamorelin inogona kuderedza zvakanyanya mudumbu VAT (avhareji kuderera kwe15-20%);
Wedzera IGF-1 mazinga uye kuvandudza metabolic mamiriro emuviri;
Kuvandudza chimiro chemuviri uye kuderedza mutoro wepfungwa unobatanidzwa nekugoverwa kwemafuta;
Haina zvakanyanya kukanganisa subcutaneous mafuta layer, bhonzo density kana tsandanyama.
2. Non-alcoholic steatohepatitis (NASH) uye chiropa fibrosis
Mishonga yemakiriniki yakaratidza kuti Tesamorelin inogona kuderedza mafuta echiropa (MRI-PDFF imaging);
Zvinotarisirwa kuvandudza hepatocyte insulin senitivity;
Inonyanya kushanda kune varwere vane HIV neNAFLD, uye ine mukana wakakura-spectrum metabolic dziviriro.
3. Metabolic syndrome uye insulin kudzivisa
Tesamorelin inoderedza zvakanyanya triglyceride mazinga uye kurema kwepamuviri;
Inovandudza HOMA-IR index uye inobatsira mukuvandudza insulin kuramba;
Zvidzidzo zvakaratidza kuti inogona kukwidziridza tsandanyama protein synthesis simba, iyo inobatsira kune vakwegura kana chirwere chisingaperi kupora.
Kugadzirwa kweAPI uye kutonga kwemhando
Iyo Tesamorelin API yakapihwa neGentolex Boka redu inotora advanced solid phase peptide synthesis tekinoroji (SPPS) uye inogadzirwa pasi peGMP nharaunda. Iine maitiro anotevera:
Kuchena ≥99% (HPLC)
Hapana endotoxin, heavy metal, yasara solvent yekuona inokodzera
Amino acid kutevedzana uye kusimbiswa kwechimiro neLC-MS/NMR
Ipa giremu-chikamu kune kilogram-level customized kugadzirwa
