plevitrexed
Plevitrexed is an orally bioavailable, small molecule, non-polyglutamatable, antifolate quinazoline derivative thymidine synthetase inhibitor with potential antineoplastic activity. This compound belongs to the class of organic compounds known as hippuric acids, which consist of a benzoyl group linked to the N-terminal of a glycine. Plevitrexed is transported into the cell via the physiological reduced folate carrier (RFC) system. Intracellularly, this agent selectively binds to the folate binding site of thymidylate synthase and inhibits thymidine synthesis, which may result in DNA synthesis inhibition and apoptosis. Plevitrexed has been investigated for use/treatment in pancreatic cancer, solid tumors, gastric cancer, lung cancer, and colorectal cancer. — NCATS
Clinical trial activity
1 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Mar 1, 2001 (NCT00014690)
Timeline
2000s
- Jan 1, 2001
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Thymidylate synthaseINHIBITOR
TYMS inhibitor
Chemistry & pharmacology
SMILES
CC1=NC(=O)C2=C(N1)C=C(C)C(CN(CC#C)C3=CC(F)=C(C=C3)C(=O)NC(CCC4=NN=NN4)C(O)=O)=C2- Mol. weight
- 532.5263 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- NCATSN094EYQ29D ↗
- ChEMBLCHEMBL126648 ↗
Also known as
- bgc9331
- plevitrexed
- plevitrexed
- plevitrexed
- zd9331
- zd 9331
- zd-9331
- zd-9331
- zd-9331
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00014690 | Phase 2 | Mar 1, 2001 | AstraZeneca |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| AstraZeneca | For profit | 1 | 1 | 1 | 2001 |