Etelcalcetide

Purogiramu inonzi Etelcalcetide

Etelcalcetideinganonyorwa, yakagadzirwacalcimimetic peptidekubvumidzwa kurapwa kweyechipiri hyperparathyroidism (SHPT)muvarwere vakuru vanechirwere cheitsvo chisingaperi (CKD)kugamuchirahemodialysis. SHPT inowanzoitika uye yakakomba dambudziko rekupedzisira-danho renal chirwere, chinokonzerwa nekukanganiswa mu calcium, phosphorus, uye vitamin D metabolism. Kuramba kukwidziridzwa kweparathyroid hormone (PTH)zvinogona kutungamirira kurenal osteodystrophy, vascular calcification, chirwere chemwoyo, uye kuwedzera kwekufa.

Etelcalcetide inopa ayakanangwa, isiri yekuvhiya sarudzokudzora mazinga ePTH muvarwere vedialysis, inomiririra yechipiri-chizvarwa calcimimetic inezvakanakira zvakasiyanapamusoro pemishonga yemuromo secinacalcet.

Nzira Yekuita

Etelcalcetide is asynthetic peptide agonistyecalcium-sensing receptor (CaSR), iri pamusoro pemasero eparathyroid gland. Inotevedzera chiito che extracellular calcium neallosterically activating CaSR, nokudaro:

• Kudzvinyirira parathyroid hormone (PTH) secretion

• Kuderedza serum calcium uye phosphorus concentrations

• Kuvandudza calcium-phosphate homeostasis

• Kuderedza njodzi yekuchinja kwemapfupa kusagadzikana uye vascular calcification

Kusiyana neoral calcimimetics, Etelcalcetide inopihwanemutsingamushure mehemodialysis, iyo inovandudza kutevedza kurapwa uye kuderedza gastrointestinal side effects.

Clinical Research uye Efficacy

Etelcalcetide yakaongororwa mune akawanda Phase 3 kiriniki miedzo, kusanganisirazvidzidzo zviviri zvakakosha zvisina kurongeka zvakadzorwarakabudiswa mukatiThe LancetuyeNew England Journal yeMishonga. Zvidzidzo izvi zvaisanganisira vanopfuura 1000 varwere vehemodialysis vane SHPT isingadzoreki.

Mhedzisiro yekiriniki yakakosha inosanganisira:

• Statistically yakakosha kuderedzwa muPTH mazinga(> 30% muruzhinji rwevarwere)

• Superior control ofserum phosphorus uye calcium-phosphate chigadzirwa (Ca × P)

• Yakakura yakazara biochemical mhinduro mazingazvichienzaniswa necinacalcet

• Zviri nani kutevedzera murwerenekuda kwekatatu-vhiki nevhiki post-dialysis IV kutonga

• Kuderedza zviratidzo zvekuchinja kwemapfupa(semuenzaniso, bone-specific alkaline phosphatase)

Aya mabhenefiti anotsigira Etelcalcetide seamutsara wekutanga injectable calcimimeticyekutarisira SHPT mune dialysis varwere.

API Kugadzira uye Hunhu

YeduPurogiramu inonzi Etelcalcetideinogadzirwa nesolid-phase peptide synthesis (SPPS), kuve nechokwadi chegoho repamusoro, kuchena, uye kugadzikana kwema molecular. Iyo API:

• Inopindirana neyakaomararaGMP uye ICH Q7 zviyero

• Inokodzera kushandiswa mukatizvinobaya zvinodhaka zvinogadzirwa

• Inopinda muyedzo wakazara wekuongorora, kusanganisira HPLC, zvakasara zvinonyungudutsa, simbi dzinorema, uye endotoxin mazinga.

• Inowanikwa mupilot uye zvekutengesa zvikero zvekugadzira

Therapeutic Potential uye Zvakanakira

• Non-hormonal treatmentyeSHPT muvarwere veCKD pane dialysis

• IV nzira inovimbisa kutevedza, kunyanya kune varwere vane mutoro wepiritsi kana GI kusashivirira

• Inogona kubatsira kuderedzamatambudziko enguva refuye mineral uye bone disorder (CKD-MBD)

• Inoenderana nephosphate binders, vhitamini D analogis, uye yakajairwa dialysis care