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

Structure

 

Show IUPAC/InChI/SMILES

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.





DRACP is developed by Dr.Zheng's team.