Raltitrexed

DCTPepD ID  DCTPepD0029

Active Ingredients   Raltitrexed

Description  A quinazoline folate analogue with antineoplastic activity. After transport into cells via the reduced folate carrier, raltitrexed undergoes intracellular polyglutamation and blocks the folate-binding site of thymidylate synthase, thereby inhibiting tetrahydrofolate activity and DNA replication and repair and resulting in cytotoxicity.

Synonyms  D1694; ICI D1694; N-(5-[N-(3,4-Dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino]-2-thenoyl)-L-glutamic Acid; N-[[5-[[(1,4-Dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-L-glutamic Acid; Tomudex; ZD1694; Raltitrexed

Disease  Advanced colorectal cancer

Classification

  

Thymidylate synthase inhibitors Amino acid and derivative

Structure Information


Molecular Formula  C21H22N4O6S

Molecular Weight  458.5

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (2S)-2-[[5-[methyl-[(2-methyl-4-oxo-3H-quinazolin-6-yl)methyl]amino]thiophene-2-carbonyl]amino]pentanedioic acid

InChI  InChI=1S/C21H22N4O6S/c1-11-22-14-4-3-12(9-13(14)19(28)23-11)10-25(2)17-7-6-16(32-17)20(29)24-15(21(30)31)5-8-18(26)27/h3-4,6-7,9,15H,5,8,10H2,1-2H3,(H,24,29)(H,26,27)(H,30,31)(H,22,23,28)/t15-/m0/s1

InChI_Key IVTVGDXNLFLDRM-HNNXBMFYSA-N

SMILES  O=C(O)[C@@H](NC(C1=CC=C(N(C)CC2=CC3=C(N=C(C)NC3=O)C=C2)S1)=O)CCC(O)=O

External Codes


PubChem CID  135400182

DrugBank Accession Number  DB00293

NCI Thesaurus Code  C1804  

UNII  FCB9EGG971   GSRS

CAS  112887-68-0



Drug approval


Drug indication
    For the treatment of malignant neoplasm of colon and rectum.

Drug Name Strength Dosage Form/Route Company Marketing Status Drug ID Approval year
Tomudex 2 mg / vial Powder For Solution; Intravenous Pfizer Canada Ulc Prescription DIN: 02229566 1996

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT03083613 Phase II Trial of Raltitrexed and Paclitaxel as Second-line Chemotherapy for Patients With Unresectable or Metastatic Gastric or Gastroesophageal Junction Adenocarcinoma Gastric Cancer; Gastroesophageal Junction Adenocarcinoma Phase 2 Treatment
NCT00004254 Phase II Study on Tomusex in Malignant Mesothelioma Malignant Mesothelioma Phase 2 Treatment
NCT05231382 A Prospective, Multicenter, Phase III Clinical Study Comparing Continuous Hepatic Arterial Infusion of Raltetrexed With Oxaliplatin(SALOX) Versus FOLFOX in Advanced Hepatocellular Carcinoma Hepatocellular Carcinoma Phase 3 Treatment
NCT02562599 Study Of Induction Chemotherapy Followed by Concurrent Chemoradiotherapy With Raltitrexed-Cisplatin for Patients With Locally Advanced Nasopharyngeal Carcinoma Nasopharyngeal Carcinoma Phase 2 Treatment
NCT03196843 Radiotherapy Combine With Raltitrexed Versus Radiotherapy Alone in Older Patients With Head and Neck Squamous Cell Carcinoma: a Prospective Randomized Controlled Trial Head and Neck Squamous Cell Carcinoma Phase 4 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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