Etelcalcetide

Etelcalcetide API

Etelcalcetideni igitabo gishyapeptide ya calcimimetikebyemewe kuvurwaicyiciro cya kabiri cya hyperparathyide (SHPT)mu barwayi bakuze bafiteindwara idakira y'impyiko (CKD)kwakirahemodialyse. SHPT ni ingorane zisanzwe kandi zikomeye zindwara zimpyiko zanyuma, ziterwa no guhungabana kwa calcium, fosifore, na vitamine D metabolism. Kuzamuka guhoraho kwaimisemburo ya parathiyide (PTH)Kuriimpyiko osteodystrophy, kubara kw'amaraso, indwara z'umutima n'imitsi, no kongera impfu.

Etelcalcetide itanga aintego, uburyo bwo kubagakugenzura urwego rwa PTH mubarwayi ba dialyse, byerekana igisekuru cya kabiri calcimimetic hamweibyiza bitandukanyehejuru yubuvuzi bwo munwa nka cinacalcet.

Uburyo bwibikorwa

Etelcalcetide ni asynthique peptide agonistBya icalcium-sensing reseptor (CaSR), iherereye hejuru ya selile ya parathiyide. Yigana ibikorwa bya calcium idasanzwe idasanzwe ikora CaSR, bityo:

• Kurwanya imisemburo ya parathiyide (PTH)

• Kugabanya calcium ya calcium na fosifore

• Kunoza calcium-fosifate homeostasis

• Kugabanya ibyago byo guhinduranya amagufwa adasanzwe no kubara imitsi

Bitandukanye na calcimimetics yo mu kanwa, Etelcalcetide iratangwaimitsinyuma ya hemodialyse, itezimbere uburyo bwo kuvura no kugabanya ingaruka za gastrointestinal.

Ubushakashatsi bwa Clinical nubushobozi

Etelcalcetide yasuzumwe mu bigeragezo byinshi byo mu cyiciro cya 3, harimobibiri by'ingenzi byateganijwe bigenzurwabyatangajwe muriLancetnaIkinyamakuru gishya cy’ubuvuzi. Ubu bushakashatsi bwarimo abarwayi ba hemodialysis barenga 1000 bafite SHPT itagenzuwe.

Ibisubizo by'ingenzi by’amavuriro birimo:

• Kugabanuka kwimibare igaragara murwego rwa PTH(> 30% mubenshi mubarwayi)

• Igenzura risumba ayandiserumu fosifore nibicuruzwa bya calcium-fosifate (Ca × P)

• Igipimo kinini cyibisubizo byibinyabuzimaugereranije na cinacalcet

• Ibyiza byo kubahiriza abarwayikubera gatatu-buri cyumweru nyuma ya dialyse IV ubuyobozi

• Kugabanuka mubimenyetso byerekana ibicuruzwa(urugero, amagufwa yihariye ya alkaline fosifata)

Izi nyungu zishyigikira Etelcalcetide nka aumurongo wambere utera inshinge calcimimeticyo gucunga SHPT mubarwayi ba dialyse.

API Gukora nubuziranenge

IwacuEtelcalcetide APIByakozwe binyuzesynthesis ikomeye ya peptide (SPPS), kwemeza umusaruro mwinshi, ubuziranenge, hamwe na molekuline itajegajega. API:

• Bihuza no gukomeraIbipimo bya GMP na ICH Q7

• Birakwiye gukoreshwa muriibikomoka ku biyobyabwenge

• Ikora isesengura ryisesengura ryuzuye, harimo HPLC, ibisigara bisigaye, ibyuma biremereye, hamwe na endotoxine

• Birashoboka muriumunzani wubucuruzi nubucuruzi

Ubuvuzi bushoboka nibyiza

• Kuvura bidasanzwekuri SHPT mu barwayi ba CKD kuri dialyse

• Inzira ya IV itanga kubahiriza, cyane cyane kubarwayi bafite umutwaro wibinini cyangwa kutihanganira GI

• Urashobora gufasha kugabanyaibibazo birebirey'imyunyu ngugu n'amagufwa (CKD-MBD)

• Bihujwe na fosifate zihuza, vitamine D igereranya, hamwe nubuvuzi busanzwe bwa dialyse