plevitrexed

Small moleculeexperimental

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

Phase 1
0
Phase 2
1
Phase 3
0
Phase 4
0

Earliest trial started Mar 1, 2001 (NCT00014690)

Timeline

2000s

  1. Jan 1, 2001

    Earliest Phase 2 Sponsor(trial)

Indications

Mechanism of action

Chemistry & pharmacology

Loading structure…

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

Also known as

  • bgc9331
  • plevitrexed
  • plevitrexed
  • plevitrexed
  • zd9331
  • zd 9331
  • zd-9331
  • zd-9331
  • zd-9331

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT00014690Phase 2Mar 1, 2001AstraZeneca
Showing 1 of 1 trials
Page 1 / 1

Organizations

Research & Development (1)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
AstraZenecaFor profit1112001
1 organizations
Page 1 / 1