Drug Information

Drug (ID: DG01515) and It's Reported Resistant Information

• Name: Brivanib
• Synonyms: Brivanib; 649735-46-6; BMS-540215; Brivanib (BMS-540215); BMS 540215; UNII-DDU33B674I; BMS540215; Brivanib [USAN]; CHEMBL377300; DDU33B674I; (2R)-1-[4-[(4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY]-5-METHYL-PYRROLO[2,1-F][1,2,4]TRIAZIN-6-YL]OXYPROPAN-2-OL; Brivanib (USAN); (R)-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-OL; (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-ol; (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo(2,1-f)(1,2,4)triazin-6-yloxy)propan-2-ol; (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol; (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol; Brivanib,BMS-540215; Brivanib (BMS540215); MLS006011288; Brivanib - BMS-540215; GTPL5671; QCR-57; SCHEMBL1227589; CHEBI:94562; DTXSID60215294; EX-A011; SYN1134; CHEBI:167686; BCPP000317; 1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol; BDBM50184807; MFCD13194684; NSC799368; s1084; ZINC13684256; AKOS015920386; AKOS015949459; BMS 540215;Unii-ddu33B674i; AC-5252; BCP9000449; CCG-268296; CS-0148; DB11958; NSC-799368; NCGC00263160-01; AS-16273; HY-10337; SMR004703038; SW219896-1; X2635; EC-000.2327; A24076; D09589; 735B466; J-500907; BRD-K28428262-001-01-7; Q27075503; (2R)-1-[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol; (r)-1-(4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol; 2-Propanol, 1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo(2,1-f)(1,2,4)triazin-6-yl)oxy)-, (2R)-
• Indication:
  In total 1 Indication(s)
  Skin infection [ICD-11: 1F28-1G0Z]; Phase 3; [1]
• Target: Bacterial 50S ribosomal RNA (Bact 50S rRNA); NOUNIPROTAC; [1]
• Formula: 5
• IsoSMILES: CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NN4C3=C(C(=C4)OC[C@@H](C)O)C
• InChI: InChI=1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1
• InChIKey: WCWUXEGQKLTGDX-LLVKDONJSA-N
• PubChem CID: 11234052
• ChEBI ID: CHEBI:94562
• TTD Drug ID: D08KBK
• DrugBank ID: DB11958

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Endometrial cancer [ICD-11: 2C76]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]

• Molecule Alteration: Missense mutation; p.S252W (c.755C>G)
• Sensitive Disease: Endometrial adenocarcinoma [ICD-11: 2C76.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: SUP-M2 cells; Colon; Homo sapiens (Human); CVCL_2209
• In Vitro Model: KARPAS-299 cells; Peripheral blood; Homo sapiens (Human); CVCL_1324
• In Vivo Model: mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.S252W (c.755C>G) in gene FGFR2 cause the sensitivity of Brivanib by unusual activation of pro-survival pathway

References

• Ref 1: Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer modelsMol Cancer Ther. 2012 Mar;11(3):690-9. doi: 10.1158/1535-7163.MCT-11-0450. Epub 2012 Jan 11.