I-Etelcalcetide

Incazelo emfushane:

I-Etelcalcetide iyi-synthetic peptide calcimimetic esetshenziselwa ukwelashwa kwe-hyperparathyroidism yesibili (SHPT) ezigulini ezinesifo sezinso esingamahlalakhona (CKD) ku-hemodialysis. Isebenza ngokuvula i-calcium-sensing receptor (CaSR) kumaseli e-parathyroid, ngaleyo ndlela yehlise amazinga e-parathyroid hormone (PTH) futhi ithuthukise umzimba wamaminerali. I-high-purity Etelcalcetide API yethu ikhiqizwa nge-solid-phase peptide synthesis (SPPS) ngaphansi kwezimo ezithobela i-GMP, ezifanele ukwakheka komjovo.

Thumela i-imeyili kithi

Imininingwane Yomkhiqizo

Omaka bomkhiqizo

I-Etelcalcetide API

I-Etelcalcetideiyinoveli, yokwenziwai-peptide ye-calcimimetickugunyazwe ukwelashwa kwei-hyperparathyroidism yesibili (SHPT)ezigulini ezindala ezineisifo sezinso esingamahlalakhona (CKD)ukwamukelahemodialysis. I-SHPT iyinkinga evamile futhi engathi sína yesifo sezinso sokuphela kwesigaba, esibangelwa ukuphazamiseka kwe-calcium, i-phosphorus, ne-vitamin D metabolism. Ukuphakama okuqhubekayo kwei-parathyroid hormone (PTH)kungaholela kui-osteodystrophy yezinso, ukubalwa kwemithambo, isifo senhliziyo nemithambo yegazi, nokwanda kokufa.

I-Etelcalcetide inikeza aokuhlosiwe, inketho engeyona yokuhlinzwaukulawula amazinga e-PTH ezigulini ze-dialysis, ezimele i-calcimimetic yesizukulwane sesibili ngeizinzuzo ezihlukenephezu kokwelashwa ngomlomo njenge-cinacalcet.

Indlela Yokwenza

I-Etelcalcetide iyi-ai-synthetic peptide agonistkwei-calcium-sensing receptor (CaSR), etholakala phezu kwamangqamuzana e-parathyroid gland. Ilinganisa isenzo se-calcium engaphandle kweseli ngokwenza i-CaSR isebenze, ngaleyo ndlela:

Ukucindezela ukukhiqizwa kwehomoni ye-parathyroid (PTH).
Ukunciphisa ukugxila kwe-calcium ne-phosphorus ku-serum
Ukwenza ngcono i-calcium-phosphate homeostasis
Ukunciphisa ingozi yokushintshashintsha kwamathambo okungavamile kanye nokubalwa kwe-vascular

Ngokungafani ne-oral calcimimetics, i-Etelcalcetide ilawulwangomjovongemva kwe-hemodialysis, eyenza ngcono ukubambelela ekwelashweni futhi inciphise imiphumela emibi yesisu.

Ucwaningo Lomtholampilo kanye Nempumelelo

I-Etelcalcetide ihlolwe ezivivinyweni eziningi zomtholampilo zeSigaba sesi-3, okuhlanganisaizifundo ezimbili ezibalulekile ezilawulwa ngokungahleliweishicilelwe kuI-LancetfuthiI-New England Journal of Medicine. Lezi zifundo zibandakanya iziguli ezingaphezu kwe-1000 ze-hemodialysis ezine-SHPT engalawulwa.

Imiphumela ebalulekile yomtholampilo ihlanganisa:

Ukwehliswa okuphawulekayo kumazinga e-PTH(ngaphezulu kuka-30% kuningi leziguli)
Ukulawula okuphezulu kwei-serum phosphorus ne-calcium-phosphate umkhiqizo (Ca × P)
Amazinga amakhulu okuphendula e-biochemicaluma kuqhathaniswa ne-cinacalcet
Ukubambelela okungcono kwesigulingenxa yokuphathwa kwe-post-dialysis IV kwamasonto amathathu
Ukwehliswa kwezimpawu zokushintshwa kwamathambo(isb, i-alkaline phosphatase eqondene nethambo)

Lezi zinzuzo zisekela i-Etelcalcetide njengeI-calcimimetic ejovayo yomugqa wokuqalayokuphatha i-SHPT ezigulini ze-dialysis.

I-API Manufacturing kanye Nekhwalithi

EyethuI-Etelcalcetide APIikhiqizwa ngei-solid-phase peptide synthesis (SPPS), okuqinisekisa isivuno esikhulu, ubumsulwa, nokuzinza kwamangqamuzana. I-API:

Ihambisana nokuqinileAmazinga e-GMP kanye ne-ICH Q7
Ilungele ukusetshenziswa kuimikhiqizo yomjovo
Ingena ekuhlolweni kokuhlaziya okuphelele, okuhlanganisa i-HPLC, izinyibilikisi ezisele, izinsimbi ezisindayo, namazinga e-endotoxin
Iyatholakala kuukulinga kanye nezikali zokukhiqiza ezentengiselwano

Amandla Okwelapha kanye Nezinzuzo

Ukwelashwa okungeyona i-hormonalye-SHPT ezigulini ze-CKD ku-dialysis
Umzila we-IV uqinisekisa ukuhambisana, ikakhulukazi ezigulini ezinomthwalo wamaphilisi noma ukungabekezelelani kwe-GI
Kungasiza ukunciphisaizinkinga zesikhathi esidei-mineral and bone disorder (CKD-MBD)
Ihambisana nezibophezelo ze-phosphate, ama-analogue kavithamini D, nokunakekelwa okujwayelekile kwe-dialysis