Raltitrexed
DRACPC ID DRACPC0029
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
Type Small Molecule
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
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.
