Drug Information

Drug (ID: DG01544) and It's Reported Resistant Information

• Name: Niraparib
• Synonyms: Niraparib; 1038915-60-4; MK-4827; (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide; ZEJULA; MK4827; UNII-HMC2H89N35; MK 4827; 2-{4-[(3s)-piperidin-3-yl]phenyl}-2h-indazole-7-carboxamide; HMC2H89N35; 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide; CHEMBL1094636; Niraparib [USAN:INN]; MK 4827 (Base); 3JD; Niraparib (USAN); Zejula (TN); MK-4827(Niraparib); GTPL8275; SCHEMBL1421875; AMY4192; DTXSID50146129; EX-A290; CHEBI:176844; MK-4827 (PARP-1); 0919AA; BDBM50316226; MFCD17779309; NSC754355; NSC800020; s2741; ZINC43206370; AKOS016004869; BCP9000940; CCG-267709; compound 56 [PMID 19873981]; CS-0780; DB11793; MK-4827/MK4827; NSC-754355; NSC-800020; ZL-2306; NCGC00346435-01; NCGC00346435-04; AC-28447; AS-35248; HY-10619; JNJ-64091742; BCP0726000077; A3617; D10140; A857972; Q25326660; 2-[4-[(3S)-3-Piperidyl]phenyl]indazole-7-carboxamide; 2-[4-(3S)-3-Piperidinylphenyl]-2H-indazole-7-carboxamide; 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]
• Indication:
  In total 1 Indication(s)
  Ewing sarcoma [ICD-11: 2B52]; .; [1]
• Target: .; NOUNIPROTAC; [1]
• Formula: 3
• IsoSMILES: C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
• InChI: InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
• InChIKey: PCHKPVIQAHNQLW-CQSZACIVSA-N
• PubChem CID: 24958200
• VARIDT ID: DR1164
• DrugBank ID: DB11793

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132H (c.395G>A)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: IDH2 cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: IDH1 cells; N.A.; Homo sapiens (Human); N.A.
• In Vivo Model: Female athymic nu/nu mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: The oncometabolite, 2-hydroxyglutarate, renders IDH1/2 mutant cancer cells deficient in homologous recombination and confers vulnerability to synthetic lethal targeting with PARP inhibitors.

References

• Ref 1: 2-Hydroxyglutarate produced by neomorphic IDH mutations suppresses homologous recombination and induces PARP inhibitor sensitivitySci Transl Med. 2017 Feb 1;9(375):eaal2463. doi: 10.1126/scitranslmed.aal2463.