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Osimertinib (AZD-9291) ntụ ntụ

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AASraw nwere nchịkọta na mmepụta site na gram ka usoro nchịkwa nke Osimertinib (AZD-9291) ntụpụ (1421373-65-0), n'okpuru usoro CGMP na usoro nchịkwa mma.

Osimertinib (AZD-9291) ntụ ntụ bụ onye na-ekwenyeghị ekwenye na-ekwenye ekwenye nke na-eme ka onye na-anabata ihe (EGFR) ghọtara na mgbanwe T790M (IC50s = 15-17 nM) ma na-egbochi ụdị ụdị anụ ọhịa ahụ (IC50 = 480 nM) .1 Ọ na-ejikọta IGF1R Ndị na - anabata HERG na ndị na - adịghị edozi ihe (IC50s = 2.9 na 16.2 μM) .1 AZD 9291 egosiputala na - egbochi ụbụrụ tumoriri na ụdị nkozi xenograft n'usoro nke 5 - 10 mg / kg na anwalela ahụike na ndị ọrịa onye na-egbuke egbuke EGFR nke na-enweghị obere ọnyá.

Product Description

Osimertinib (AZD-9291) uzuzu uzuzu


Osimertinib (AZD-9291) ntụ ntụ isi agwa

aha: Osimertinib (AZD-9291) ntụ ntụ
CAS: 1421373-65-0
Molekụla Formula: C28H33N7O2
Ọbara arọ: 499.61
Melt Point: > 188ºC
Nchekwa Nche: -20 ° C
agba: Uzuzu uzuzu siri ike


Osimertinib (AZD-9291) ntụ ntụ na ojiji

aha

AZD-9291 powder (CAS 1421373-65-0), N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide

AZD-9291 Njikere ntụ ntụ

AZD-9291 uzuzu a na-edozi otu ugboro kwa ụbọchị na 5 mg / kg mere ka ọnụ ọgụgụ dị ukwuu nke etuto ahụ gafee EGFRm + (PC9; 178% inhibition) na EGFRm + / T790M (H1975; 119% growthhibition)
mgbe 14 ụbọchị dosing. Na 5 mg / kg AZD-9291 ntụ ntụ zuru ezu iji mee ka ọ dị ntakịrị shrinkage nke EGFRm + na EGFRm + / T790M transgenic mouse pulmon. Ejikọtara ọgwụ mgbochi tumor na nkwupụta miri emi nke EGFR phosphorylation na ụzọ ụzọ mgbagwoju anya dị ka AKT na ERK. Ogologo oge ọgwụgwọ nke PC9 na H1975 xenograft tumors na ngwongwo AZD-9291 na-eduga nzaghachi macroscopic zuru ezu, nke na-enweghị nsụgharị anya mgbe 40 gasịrị na-agbado, ma na-echere karịa 100 ụbọchị. Ọzọkwa, data ndị na-ebute ihe na-egosi na AZD-9291 ntụ ntụ nwere ike ịchekwa ụbụrụ nke nwere nkwụsi ike na usoro HER2-amplification a na-adịbeghị anya, nke a nwere ike ịgbatị uru ya na ntanetị na-akwado ndị ọrịa.

Ịdọ aka ná ntị na ntụ ntụ AZD-9291

Azu nke AZD-9291 (CAS 1421373-65-0) bụ naanị ọgwụ a kwadoro maka ndị ọrịa na-enwe mmerụ nke EGFR T790M na-adịghị mma. E gosipụtara ihe ngosi a n'okpuru usoro mmemme amara nke FDA nke dabeere na usoro nzaghachi tumọ na oge nke nzaghachi (DoR).

Ihe ndị na-emetụta ụbụrụ na-agụnye afọ ọsịsa, stomatitis, rashes, akọrọ ma ọ bụ akpụkpọ anụ, ọrịa ebe mkpịsị aka ma ọ bụ nkedo abutụ akpụkpọ ahụ, obere ala platelet, ọnụ ọgụgụ dị ala, na obere neutrophil.
Enweghị nkwenye maka TAGRISSO
Ọrịa Na-akpata Mkpụrụ Ọkụ Interstitial (ILD) / Pneumonitis mere na 3.3% ma nwụọ na 0.5% nke ndị ọrịa 813 TAGRISSO. Debe TAGRISSO ma chọpụta maka ILD n'oge ọ bụla na-arịa ọrịa na-egosi ọrịa ILD (dịka, dyspnea, ụkwara na ahụ ọkụ). Mee ka TAGRISSO kwụsị ma ọ bụrụ na ILD kwadoro
Mgbatị oge QTc mere na ndị ọrịa TAGRISSO. N'ime ndị ọrịa 411 na ọmụmụ abụọ nke Phase II, otu onye ọrịa (0.2%) hụrụ na ọ nwere QTc karịa 500 msec, na ọrịa 11 (2.7%) nwere mmụba si QTc dị elu karịa 60 msec. Ọ bụrụ na ndị na-arịa ọrịa na-arụ ọrụ mgbe niile na ECG na electrolytes na ndị ọrịa na-enwe ogologo oge QTc, ọrịa obi congestive, ihe mgbagwoju anya, ma ọ bụ ndị na-aṅụ ọgwụ maara ogologo oge. Kwụsị mgbe niile TAGRISSO na ndị ọrịa na-etolite QTc nkeji oge na ihe ịrịba ama / mgbaàmà nke ndụ egwu arrhythmia
Cardiomyopathy mere na 1.4% ma gbuo na 0.2% nke 813 TAGRISSO ọrịa. Onu ogugu uzo efu nke aka ekpe (LVEF) gbadaa> 10% na dobe ka <50% mere na 2.4% nke (9 / 375) TAGRISSO. Nyocha LVEF tupu nmalite na mgbe ahụ na oge elekere 3 nke ọgwụgwọ. Debe TAGRISSO ma ọ bụrụ na ọnụọgụ nke ejection decreased by 10% si na ọnụahịa nke pretreatment ma ọ bụ ihe na-erughị 50%. Maka mgbagha obi mgbaàmà nke mgbagwoju anya ma ọ bụ ịnọgide na-arụ ọrụ nkwụsị LV na-adịghị edozi n'ime izu 4, kwụsịtụ TAGRISSO.
Nye ndị inyom dị ime ndụmọdụ ka ha nwee ike inwe nwa ebu n'afọ. Gwa ụmụ nwanyị ndụmọdụ maka ịmụ nwa iji ọgwụ mgbochi dị irè n'oge ọgwụ TAGRISSO na maka izu 6 mgbe ụgwụ ikpeazụ gasịrị. Nye ụmụ nwoke ndụmọdụ na ndị mmekọ nwanyị nwere ike ịmụ nwa iji mepụta ọgwụ mgbochi dị irè maka ọnwa 4 mgbe ụgwụ ikpeazụ gasịrị.
Mmeghachi omume kachasị njọ (> 20%) hụrụ na ndị ọrịa TAGRISSO bụ afọ ọsịsa (42%), ọkụ ọkụ (41%), akpụkpọ anụ (31%) na ngbu toxicity (25%).

Ntuziaka ọzọ

Azu nke AZD-9291 na-arụsi ọrụ ike na ndị ọrịa nwere ọrịa kansa na-egbu anụ na nnwere onwe EGFR T790M bụ ndị nwere ọrịa na-aga n'ihu n'oge ọgwụgwọ na ndị na-eme ihe nchịkwa EGFR tyrosine kinase.

A na-amụ ntụle AZA-9291 na ule nkwenye ahụ, AURA3, akwukwọ a na-emeghe, usoro ọmụmụ nke Phase nke atọ a tụlere iji rụọ ọrụ na nchedo nke AZD-9291 ntụ ntụ na doublet chemotherapy dabeere na platinum na ndị nwere ọrịa EGFR T790M, ma ọ bụ NSCLC metastatic ndị na-enwe ọganihu na-esote tupu usoro ọgwụ na EGFR-TKI. A na-enyochakwa ntụ ntụ AZD-9291 na ọnọdụ adjuvant na n'usoro nhazi mbụ nke metastatic, gụnyere ndị ọrịa nwere metastases ụbụrụ, nakwa dịka ya na akụkụ ndị ọzọ.

Mbadamba AZD-9291 powder 80mg otu ugboro kwa ụbọchị bụ ọgwụ mbụ e gosipụtara maka ọgwụgwọ nke ndị ọrịa na-emepụta ihe na-eme ka onye nabatara (EGFR) nke T790M bụ nke na-abụghị obere obere cell cancer (NSCLC), dịka onye FDA ule, ndị nwere ọganihu na ma ọ bụ mgbe EGFR tyrosine kinase inhibitor (TKI) ọgwụgwọ. Ihe omumu omumu na vitamin na-egosi na AZD-9291 uzuzu nwere oke ike na mmechi ihe megide EGFR phosphorylation di iche iche na-achoputa na EGFRm na T790M mutant NSCLC na enweghi mmekorita megide EGFR n'igwe uzo.

Ọ bụ Òtù Na-ahụ Maka Ahụ Ike Ụwa (WHO) bipụtara Osimertinib ugbua dị ka Nkwepụta Na-abụghị Nhọrọ International (INN) nke a chọrọ maka ntụ ọka AZD-9291, ọ pụkwara ịmalite nke ọma na November 2015. Na US, American Medical Association kwetara Osimertinib ntụ ntụ dịka United States Adoped Name (USAN).

AZD-9291 Powder (CAS 1421373-65-0)

Min iji 10grams.
Ajuju ajuju nke di n'ogo (N'ime 1kg) nwere ike iziputa na 12 awa mgbe ugwo.
Maka usoro ka ukwuu (N'ime 1kg) nwere ike zipụ na 3 ụbọchị ọrụ mgbe ịkwụ ụgwọ.

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