Drug Information

Drug (ID: DG01625) and It's Reported Resistant Information

• Name: Ivosidenib
• Synonyms: Ivosidenib; 1448347-49-6; AG-120; Tibsovo; AG120; UNII-Q2PCN8MAM6; Q2PCN8MAM6; (2S)-N-[(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl]-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide; (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide; RG120; ivosidenibum; (2S)-N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide; Ivosidenib [INN]; Tibsovo (TN); Ivosidenib [USAN]; Ivosidenib [WHO-DD]; Ivosidenib (USAN/INN); Ivosidenib [USAN:INN]; GTPL9217; CHEMBL3989958; SCHEMBL15122512; EX-A992; CHEBI:145430; BDBM363689; AMY38924; US9850277, Compound 176; MFCD29036964; NSC789102; s8206; ZINC205136523; CCG-270141; CS-5122; DB14568; NSC-789102; NCGC00476170-04; NCGC00476170-06; (S)-N-((S)-1-(2-chlorophenyl)-2-(3,3-difluorocyclobutylamino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-; AC-32624; AS-35058; HY-18767; A14386; D11090; A900315; Q27895417; (2S)-1-(4-Cyano-2-pyridinyl)-5-oxo-L-prolyl-2-(2-chloroPh)-N-(3,3-difluorocyclobutyl)-N2-(5-fluoro-3-pyridinyl)-glycinamide; (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide;AG-120; (S)-N-((S)-1-(2-chlorophenyl)-2-(3,3-difluorocyclobutylamino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide; Glycinamide, 1-(4-cyano-2-pyridinyl)-5-oxo-L-prolyl-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-N2-(5-fluoro-3-pyridinyl)-, (2S)-; N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxo-L-prolinamide
• Indication:
  In total 3 Indication(s)
  Cholangiocarcinoma [ICD-11: 2C12]; Approved; [1]
  Multiple myeloma [ICD-11: 2A83]; Approved; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Approved; [1]
• Target: Fibroblast growth factor (FGF); NOUNIPROTAC; [1]
• Target: Fibroblast growth factor receptor (FGFR); NOUNIPROTAC; [1]
• Formula: 7
• IsoSMILES: C1CC(=O)N([C@@H]1C(=O)N(C2=CC(=CN=C2)F)[C@@H](C3=CC=CC=C3Cl)C(=O)NC4CC(C4)(F)F)C5=NC=CC(=C5)C#N
• InChI: InChI=1S/C28H22ClF3N6O3/c29-21-4-2-1-3-20(21)25(26(40)36-18-11-28(31,32)12-18)37(19-10-17(30)14-34-15-19)27(41)22-5-6-24(39)38(22)23-9-16(13-33)7-8-35-23/h1-4,7-10,14-15,18,22,25H,5-6,11-12H2,(H,36,40)/t22-,25-/m0/s1
• InChIKey: WIJZXSAJMHAVGX-DHLKQENFSA-N
• PubChem CID: 71657455
• ChEBI ID: CHEBI:145430
• TTD Drug ID: D01ZLU
• INTEDE ID: DR00362
• DrugBank ID: DB14568

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Acute myeloid leukemia [ICD-11: 2A60]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132C (c.394C>T)
• Sensitive Disease: Acute myeloid leukemia [ICD-11: 2A60.0]
• Experimental Note: Identified from the Human Clinical Data

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132S (c.394C>A)
• Sensitive Disease: Acute myeloid leukemia [ICD-11: 2A60.0]
• Experimental Note: Identified from the Human Clinical Data

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132G (c.394C>G)
• Sensitive Disease: Acute myeloid leukemia [ICD-11: 2A60.0]
• Experimental Note: Identified from the Human Clinical Data

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132H (c.395G>A)
• Sensitive Disease: Acute myeloid leukemia [ICD-11: 2A60.0]
• Experimental Note: Identified from the Human Clinical Data

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132L (c.395G>T)
• Sensitive Disease: Acute myeloid leukemia [ICD-11: 2A60.0]
• Experimental Note: Identified from the Human Clinical Data

References

• Ref 1: Durable Remissions with Ivosidenib in IDH1-Mutated Relapsed or Refractory AMLN Engl J Med. 2018 Jun 21;378(25):2386-2398. doi: 10.1056/NEJMoa1716984. Epub 2018 Jun 2.