Brivanib Alaninate
DRACPC ID DRACPC0089
Active Ingredients Brivanib Alaninate
Description The alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor Brivanib with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression.
Synonyms BMS-582664; Brivanib Alaninate; BMS582664; BMS 582664
Type Small Molecule
Disease Colorectal Cancer
Classification
VEGFR2 inhibitor Amino acid and derivative Antiangiogenesis agent
Structure Information
Molecular Formula C22H24FN5O4
Molecular Weight 441.5
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name (2R)-1-({4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl}oxy)propan-2-yl (2S)-2-aminopropanoate
InChI InChI=1S/C22H24FN5O4/c1-11-7-15-16(27-11)5-6-17(19(15)23)32-21-20-13(3)18(8-28(20)26-10-25-21)30-9-12(2)31-22(29)14(4)24/h5-8,10,12,14,27H,9,24H2,1-4H3/t12-,14+/m1/s1
InChI_Key LTEJRLHKIYCEOX-OCCSQVGLSA-N
SMILES CC1=CC2=C(N1)C=CC(OC3=NC=NN4C3=C(C)C(OC[C@@H](C)OC([C@@H](N)C)=O)=C4)=C2F
External Codes
PubChem CID 11154925
DrugBank Accession Number DB11865
NCI Thesaurus Code C53397
UNII U2Y5OFN795 GSRS
CAS 649735-63-7
Drug approval
Drug indication
Brivanib alaninate has been investigated for the treatment of Colorectal Cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT01267253 | A Phase II Evaluation of Brivanib (BMS582664) in the Treatment of Persistent or Recurrent Carcinoma of the Cervix (BMS Study CA182-048) | Cervical Adenocarcinoma; Cervical Adenosquamous Carcinoma; Cervical Squamous Cell Carcinoma, Not Otherwise Specified; Persistent Disease; Recurrent Cervical Carcinoma | Phase 2 | Treatment |
| NCT04212221 | A Multicenter, Open-label, Phase I/II Dose Escalation and Expansion Clinical Study to Assess the Safety and Efficacy of MGD013 Monotherapy and in Combination With Brivanib Alaninate (ZL-2301) in Patients With Advanced Liver Cancer | Advanced Hepatocellular Carcinoma (HCC) | Phase 1/2 | Treatment |
| NCT00437437 | Phase I Study to Determine the Effect of a High Fat Meal on the Pharmacokinetics of BMS-540215, the Active Metabolite of Brivanib Alaninate in Subjects With Advanced or Metastatic Solid Tumors | Tumors | Phase 1 | Treatment |
| NCT03516071 | A Multicenter, Randomized, Open-label, Phase II Clinical Study to Evaluate the Efficacy and Safety of Brivanib Alaninate (ZL-2301) Combined With Best Supportive Care (BSC) and Pharmacokinetic Profiles of Brivanib Alaninate in Patients With Advanced Hepatocellular Carcinoma (HCC) Failed or Intolerant of Standard Systemic Chemotherapy and/or Sorafenib | Hepatocellular Carcinoma (HCC) | Phase 2 | Treatment |
| NCT03895788 | An Open-Label, Single-Arm, Phase I Clinical Trial to Evaluate the Safety and Tolerability of ZL-2306 (Niraparib) in Combination With Brivanib in Patients With Recurrent Ovarian Cancer | Ovarian Cancer | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
