Pemetrexed Disodium

한글명:Pemetrexed Disodium

카스 번호150399-23-8

상품명:Pemetrexed Disodium

CBNumberCB4385473

분자식C20H22N5NaO6

포뮬러 무게451.41

MOL 파일150399-23-8.mol

화학적 성질

녹는점	254-258°C (dec.)
저장 조건	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
용해도	에 용해됨메탄올, 물
물리적 상태	고체
물리적 상태	단단한 모양
색상	회백색
안정성	흡습성
InChIKey	UTEALKYVANXUSG-NVZXTOETNA-N
SMILES	C(C1=CNC2NC(N)=NC(=O)C1=2)CC1C=CC(C(=O)N[C@H](C(=O)O)CCC(=O)O)=CC=1.[NaH] \|&1:20,r\|
CAS 데이터베이스	150399-23-8(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기	T;Xi,Xi,T
위험 카페고리 넘버	36/38-60-61-68
안전지침서	36/37/39-53

그림문자(GHS)

Pemetrexed Disodium 화학적 특성, 용도, 생산

화학적 성질
Crystalline Solid
정의
ChEBI: An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 4 1 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).
일반 설명
The drug is available in a 100-mg sterile vial for IV use. Thedrug appears to be effective against a range of tumors includingmesothelioma, NSCLC, colorectal cancer, bladdercancer, and lung cancer. The mechanism of action involvesinhibition of TS resulting in inhibition of thymidylate andDNA synthesis. This drug is a pyrrolopyrimidine analog offolate with antifolate activity. Resistance can occur by increasedexpression of TS, decreased binding affinity for TS,or decreased drug transport into cells. The drug is administeredonly via the IV route and distributes to all tissues.Cellular activation to the more potent polyglutamated formsoccurs, and the majority of the dose is excreted unchangedin the urine. The drug interaction and toxicity profiles aresimilar to that of methotrexate.
Mechanism of action
Like methotrexate, it is actively transported into tumor cells through reduced folate carriers and, in polyglutamated form, inhibits the synthesis of pyrimidine and purine-based nucletotides by disrupting folatedependent metabolic processes . In addition to DHFR, this pyrrolopyrimidine-based inhibitor binds tightly to thymidylate synthase and GAR transformylase.
Clinical Use
Pemetrexed is a novel multitarget antifolate used by the IV route for the treatment of advanced or metastatic nonsmall cell lung cancer and in combination with cisplatin in malignant pleural mesothelioma.
부작용
Patients on pemetrexed must take folate and vitamin B12 supplements to reduce the risk of bone marrow suppression (neutropenia, thrombocytopenia, and anemia) and GI side effects. Pretreatment with corticosteroids can reduce the risk of drug-induced skin rash. Pemetrexed has a half-life of 3.5 hours and is excreted primarily unchanged via the kidneys. Significant cross-resistance has been noted between pemetrexed and other pyrimidine and folate antagonists.

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