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QuickView for raltitrexed (compound)


PubChem
Name: raltitrexed
PubChem Compound ID: 104758
Molecular formula: C21H22N4O6S
Molecular weight: 458.489 g/mol
Synonyms:
ZD1694; ZN-D1694; L-Glutamic acid, N-((5-(((1,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl)methylamino)-2-thienyl)carbonyl)-; Raltitrexed (JAN/USAN); ZD-1694; (S)-2-[(1-{5-[Methyl-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-amino]-thiophen-2-yl}-methanoyl)-amino]-pentanedioic acid; AIDS106596; D01064; Raltitrexed; D1694.
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DrugBank
Identification
Name: raltitrexed
Name (isomeric): DB00293
Drug Type: small molecule
Synonyms:
ZD1694; ZD-1694
Brand: Tomudex
Category: Antimetabolites, Antimetabolites, Antineoplastic, Antineoplastic Agents, Enzyme Inhibitors, Folic Acid Antagonists
CAS number: 112887-68-0
Pharmacology
Indication: For the treatment of malignant neoplasm of colon and rectum
Pharmacology:
Raltitrexed belongs to a group of medicines known as antimetabolites. It is used to treat cancer of the colon and rectum. It may also be used to treat other kinds of cancer, as determined by your doctor. Raltitrexed blocks an enzyme needed by the cell to live. This interferes with the growth of cancer cells, which are eventually destroyed. Since th...
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Mechanism of Action:
Raltitrexed is an antineoplastic Agents and folic acid antagonists. Raltitrexed inhibits thymidylate synthase (TS) leading to DNA fragmentation and cell death. It is transported into cells via a reduced folate carrier. Inside the cell Raltitrexed is extensively polyglutamated, which enhances thymidylate synthase inhibitory power and duration. Inhib...
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Protein binding: >93%
Biotransformation: Raltitrexed is transported into cells via a reduced folate carrier. Inside the cell it is extensively polyglutamated by the enzyme folyl polyglutamate synthetase to polyglutamate forms.
Half Life: 198 hours
Toxicity: Side effects include pale skin, troubled breathing, unusual bleeding or bruising, unusual tiredness or weakness, black, tarry stools, chest pain, chills, cough, fever, painful or difficult urination, shortness of breath, sore throat, sores, ulcers, or white spots on lips or in mouth, swollen glands, increase in bowel movements, loose stools, soft stools.
Affected organisms: Humans and other mammals

Targets