Tesamorelin
Tesamorelin API
Tesamorelin ndi mankhwala a peptide opangidwa, dzina lonse ndi ThGRF (1-44) NH₂, yomwe ndi analog ya kukula kwa hormone (GHRH). Imalimbikitsa anterior pituitary kuti itulutse hormone ya kukula (GH) poyerekezera zochita za GHRH yokhazikika, motero imawonjezera mosadukiza mlingo wa insulini-monga kukula factor 1 (IGF-1), kubweretsa mndandanda wa zopindulitsa mu metabolism ndi kukonza minofu.
Pakadali pano, Tesamorelin yavomerezedwa ndi a FDA kuti azichiza lipodystrophy yokhudzana ndi kachilombo ka HIV, makamaka kuti achepetse kuchuluka kwa mafuta m'mimba (visceral adipose tissue, VAT). Zaphunziridwanso kwambiri za **anti-aging, metabolic syndrome, non-alcoholic fatty hever disease (NAFLD/NASH)** ndi madera ena, kusonyeza chiyembekezo chachikulu chogwiritsira ntchito.
Njira yochitira
Tesamorelin ndi 44-amino acid peptide yokhala ndi mawonekedwe ofanana kwambiri ndi GHRH yachilengedwe. Njira yake yochitira zinthu ndi:
Yambitsani GHRH receptor (GHRHR) kuti mulimbikitse anterior pituitary kutulutsa GH.
GH ikakwera, imagwira ntchito pachiwindi ndi minyewa yozungulira kuti iwonjezere kaphatikizidwe ka IGF-1.
GH ndi IGF-1 amatenga nawo gawo mu metabolism yamafuta, kaphatikizidwe ka mapuloteni, kukonza ma cell ndi kukonza kachulukidwe ka mafupa.
Imagwira makamaka pakuwonongeka kwamafuta a visceral (kuphatikiza mafuta) ndipo imakhala ndi mphamvu zochepa pamafuta a subcutaneous.
Poyerekeza ndi jekeseni yachindunji ya GH, Tesamorelin imalimbikitsa kutsekemera kwa GH kupyolera mu njira zowonongeka, zomwe zimakhala pafupi ndi chikhalidwe cha thupi ndipo zimapewa zovuta zomwe zimachitika chifukwa cha GH yambiri, monga kusunga madzi ndi insulini kukana.
Kafukufuku ndi mphamvu zachipatala
Kuchita bwino kwa Tesamorelin kwatsimikiziridwa kudzera mu mayesero angapo azachipatala, makamaka m'madera otsatirawa:
1. Lipodystrophy yokhudzana ndi HIV (zizindikiro zovomerezeka ndi FDA)
Tesamorelin ikhoza kuchepetsa kwambiri VAT ya m'mimba (kuchepa kwapakati pa 15-20%);
Wonjezerani milingo ya IGF-1 ndikuwongolera kagayidwe kachakudya m'thupi;
Kupititsa patsogolo mawonekedwe a thupi ndikuchepetsa mtolo wamaganizo wokhudzana ndi kugawanso mafuta;
Simakhudza kwambiri subcutaneous mafuta wosanjikiza, kachulukidwe mafupa kapena minofu misa.
2. Steatohepatitis yopanda mowa (NASH) ndi chiwindi fibrosis
Mayesero achipatala asonyeza kuti Tesamorelin ikhoza kuchepetsa mafuta a chiwindi (MRI-PDFF imaging);
Akuyembekezeka kukulitsa chidwi cha hepatocyte insulin;
Ndiwothandiza makamaka kwa odwala omwe ali ndi kachilombo ka HIV ndi NAFLD, ndipo ali ndi chitetezo chochuluka cha metabolic.
3. Metabolic syndrome ndi insulin kukana
Tesamorelin imachepetsa kwambiri milingo ya triglyceride ndi kunenepa kwambiri m'mimba;
Imawongolera index ya HOMA-IR ndikuthandizira kukonza kukana kwa insulini;
Kafukufuku wasonyeza kuti akhoza kulimbikitsa minofu kaphatikizidwe mapuloteni mphamvu, amene n'kopindulitsa kwa okalamba kapena matenda aakulu kuchira.
Kupanga kwa API ndi kuwongolera khalidwe
Tesamorelin API yoperekedwa ndi Gulu lathu la Gentolex imatenga ukadaulo wokhazikika wa peptide synthesis (SPPS) ndipo imapangidwa pansi pa chilengedwe cha GMP. Lili ndi izi:
Kuyera ≥99% (HPLC)
Palibe endotoxin, heavy metal, kudziwika kotsalira kwa zosungunulira koyenera
Tsatanetsatane wa amino acid ndi kutsimikizira kapangidwe ka LC-MS/NMR
Perekani zopanga makonda za gilamu mpaka kilogalamu
