Tesamorelin

Tesamorelin API

I-Tesamorelin iyisiyobisi se-peptide yokwenziwa, igama elipheleleyo yi-ThGRF (1-44) NH₂, okuyi-hormone yokukhula ekhupha i-hormone (GHRH) analog. Ivuselela i-pituitary yangaphambili ukuba ikhuphe i-hormone yokukhula (GH) ngokufanisa isenzo se-GHRH engapheliyo, ngaloo ndlela inyusa ngokungangqalanga inqanaba le-insulin-like ukukhula factor 1 (IGF-1), ukuzisa uthotho lweenzuzo kwimetabolism kunye nokulungiswa kwezicubu.

Okwangoku, i-Tesamorelin ivunyiwe yi-FDA yonyango lwe-lipodystrophy enxulumene ne-HIV, ngakumbi ekunciphiseni ukuqokelelwa kwamafutha e-visceral esiswini (i-visceral adipose tissue, i-VAT). Kwakhona kuye kwafundwa ngokubanzi ** ukulwa nokuguga, i-syndrome ye-metabolic, isifo se-fatty non-alcoholic fat (NAFLD / NASH) ** kunye nezinye iinkalo, ezibonisa amathuba okusetyenziswa okubanzi.
Indlela yokwenza

I-Tesamorelin yi-44-amino acid peptide enesakhiwo esifana kakhulu ne-GHRH yendalo. Indlela yokusebenza kwayo yile:

Vula i-GHRH receptor (GHRHR) ukuvuselela i-pituitary yangaphambili ukukhulula i-GH.

Emva kokuba i-GH iphakanyisiwe, isebenza kwisibindi kunye nezicubu ezijikelezayo ukwandisa i-IGF-1 synthesis.

I-GH kunye ne-IGF-1 ngokudibeneyo bathatha inxaxheba kwi-fat metabolism, i-protein synthesis, ukulungiswa kweeseli kunye nokugcinwa kwamathambo.

Isebenza ikakhulu kwi-visceral fat decomposition (ukuhlanganiswa kwamafutha) kwaye inefuthe elincinci kumafutha angaphantsi.

Xa kuthelekiswa ne-exogenous injection ye-GH, i-Tesamorelin ikhuthaza ukukhutshwa kwe-GH ngokusebenzisa iindlela ezingapheliyo, ezikufutshane nesigqi somzimba kwaye zigweme ukusabela okubi okubangelwa yi-GH eninzi, njengokugcinwa kwamanzi kunye nokuxhatshazwa kwe-insulin.

Uphando kunye nokusebenza kweklinikhi

Ukusebenza kweTesamorelin kuye kwaqinisekiswa ngezilingo ezininzi zeklinikhi, ngakumbi kwezi ndawo zilandelayo:

1. I-lipodystrophy enxulumene ne-HIV (imiqondiso evunywe yi-FDA)

I-Tesamorelin inokunciphisa kakhulu i-VAT yesisu (i-avareji yokuncipha kwe-15-20%);

Ukwandisa amanqanaba e-IGF-1 kunye nokuphucula imeko ye-metabolic yomzimba;

Ukuphucula ukumila komzimba kunye nokunciphisa umthwalo wengqondo ohambelana nokusabalalisa kwamafutha;

Ayichaphazeli kakhulu i-subcutaneous fat layer, ukuxinana kwamathambo okanye ubunzima bemisipha.

2. I-steatohepatitis engeyiyo utywala (NASH) kunye ne-fibrosis yesibindi

Izilingo zeklinikhi zibonise ukuba iTesamorelin inokunciphisa umxholo weoli yesibindi (i-MRI-PDFF imaging);

Kulindeleke ukuba kuphuculwe uvakalelo lwe-insulin ye-hepatocyte;

Isebenza ngokukodwa kwizigulane ezine-HIV kunye ne-NAFLD, kwaye inokhuseleko olubanzi lwe-metabolic.

3. I-Metabolic syndrome kunye nokuxhatshazwa kwe-insulin

I-Tesamorelin iyanciphisa kakhulu amanqanaba e-triglyceride kunye nokukhuluphala kwesisu;

Ukuphucula isalathisi se-HOMA-IR kwaye inceda ekuphuculeni ukuxhathisa kwe-insulin;

Uphononongo lubonise ukuba lunokuphucula umthamo weprotheyini ye-muscle synthesis, enenzuzo kubantu abadala okanye ukubuyiswa kwezifo ezingapheliyo.

Ukuveliswa kwe-API kunye nokulawula umgangatho

I-Tesamorelin API enikezelwa liQela lethu leGentolex lithatha iteknoloji ye-peptide synthesis yesigaba esiqinileyo (SPPS) kwaye iveliswa phantsi kwemeko ye-GMP. Inezi mpawu zilandelayo:

Ubunyulu ≥99% (HPLC)
Akukho i-endotoxin, isinyithi esinzima, ukufunyanwa kwe-solvent eyintsalela efanelekile
Ukulandelelana kwe-amino acid kunye nokuqinisekiswa kwesakhiwo nge-LC-MS / NMR
Ukubonelela nge-gram-level ukuya kwikhilogram-level yemveliso eyenziwe ngokwezifiso