Etelcalcetide

Etelcalcetide API

Etelcalcetideke padi, ya maiketsetsopeptide ea calcimimetice amohetsoeng bakeng sa phekolo eahyperparathyroidism ea bobeli (SHPT)ho bakuli ba baholo ba nang lelefu le sa foleng la liphio (CKD)ho amohelahemodialysis. SHPT ke bothata bo tloaelehileng le bo tebileng ba lefu la renal la ho qetela, le bakoang ke ho senyeha ha metabolism ea calcium, phosphorus le vithamine D. Phahamiso e phehellang eahormone ea parathyroid (PTH)ka lebisa hoRenal osteodystrophy, vascular calcification, lefu la pelo le methapo ea mali, le ho eketseha ha lefu.

Etelcalcetide e fana kakhetho e lebisitsoeng, e seng ea ho buoaho laola maemo a PTH ho bakuli ba dialysis, ba emelang calcimimetic ea moloko oa bobeli kamelemo e ikhethangka liphekolo tsa molomo tse kang cinacalcet.

Mokhoa oa Ts'ebetso

Etelcalcetide keagonist ea maiketsetso ea peptidetsakhalsiamo-sensing receptor (CaSR), e ka holim'a lisele tsa tšoelesa ea parathyroid. E etsisa ketso ea extracellular calcium ka ho etsa allosterically activate CaSR, ka tsela eo:

• Ho fokotsa tlhahiso ea hormone ea parathyroid (PTH).

• Ho fokotsa khatello ea serum calcium le phosphorus

• Ho ntlafatsa calcium-phosphate homeostasis

• Ho fokotsa kotsi ea ho ba le mathata a ho fetoha ha masapo le calcification ea vascular

Ho fapana le oral calcimimetics, Etelcalcetide e tsamaisoaka methapoka mor'a hemodialysis, e ntlafatsang ho khomarela kalafo le ho fokotsa litla-morao tsa mala.

Lipatlisiso tsa Tleliniki le Katleho

Etelcalcetide e hlahlobiloe litekong tse ngata tsa Mokhahlelo oa 3, ho kenyeletsoalithuto tse peli tsa bohlokoa tse laoloang ka tšohanyetsoe hatisitsoeng kaThe LancetleNew England Journal of Medicine. Lithuto tsena li ne li kenyelletsa bakuli ba fetang 1000 ba hemodialysis ba nang le SHPT e sa laoleheng.

Liphello tsa bohlokoa tsa kliniki li kenyelletsa:

• Phokotso ea bohlokoa ka lipalo maemong a PTH(> 30% ho bongata ba bakuli)

• Taolo e phahameng easerum phosphorus le sehlahisoa sa calcium-phosphate (Ca × P)

• Litefiso tse kholo ka kakaretso tsa karabelo ea biochemicalha e bapisoa le cinacalcet

• Ho khomarela mokuli hamolemoka lebaka la tsamaiso ea IV ea post-dialysis ea libeke tse tharo

• Phokotso ea matšoao a phetoho ea masapo(mohlala, alkaline phosphatase e khethehileng lesapong)

Melemo ena e tšehetsa Etelcalcetide joalo kacalcimimetic ea mothapo oa pelebakeng sa ho laola SHPT ho bakuli ba dialysis.

API Manufacturing le Quality

Tsa ronaEtelcalcetide APIe etsoa kasolid-phase peptide synthesis (SPPS), ho netefatsa chai e ngata, bohloeki, le botsitso ba limolek'hule. API:

• E lumellana le stringentLitekanyetso tsa GMP le ICH Q7

• E loketse ho sebelisoa holihlahisoa tsa lithethefatsi tse nang le ente

• E etsa tlhahlobo e felletseng ea tlhahlobo, ho kenyeletsoa HPLC, li-solvents tse setseng, litšepe tse boima, le maemo a endotoxin.

• E fumaneha hosekala sa tlhahiso ea lifofane le khoebo

Matla a Phekolo le Melemo

• Kalafo e seng ea li-hormonebakeng sa SHPT ho bakuli ba CKD ka dialysis

• Tsela ea IV e netefatsa hore ho latela melao, haholo-holo ho bakuli ba nang le moroalo oa lipilisi kapa ho se mamelle GI

• E ka thusa ho fokotsamathata a nako e telelebothata ba liminerale le masapo (CKD-MBD)

• E lumellana le li-binder tsa phosphate, li-analogue tsa vithamine D, le tlhokomelo e tloaelehileng ea dialysis