Drug Information

Drug (ID: DG01556) and It's Reported Resistant Information

• Name: Apitolisib
• Synonyms: Apitolisib; 1032754-93-0; GDC-0980; GDC0980; RG7422; GNE 390; (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one; GDC-0980 (Apitolisib); UNII-1C854K1MIJ; RG 7422; GDC-0980 (RG7422); GDC 0980; 1C854K1MIJ; CHEMBL1922094; Apitolisib (GDC-0980, RG7422); RG-7422; (2s)-1-(4-{[2-(2-Aminopyrimidin-5-Yl)-7-Methyl-4-(Morpholin-4-Yl)thieno[3,2-D]pyrimidin-6-Yl]methyl}piperazin-1-Yl)-2-Hydroxypropan-1-One; C23H30N8O3S; (2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one; (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one.; GNE 390; GDC 0980; RG 7422; Apitolisib [USAN:INN]; Apitolisib (USAN/INN); Apitolisib(GDC-0980); Gne-390; Apitolisib (GDC-0980); SCHEMBL466297; GTPL7888; DTXSID50145738; EX-A041; QCR-182; SYN1150; AOB87742; BCP02622; BDBM50358204; GDC-0980,RG7422; GDC0980(RG7422); MFCD20274520; NSC764091; NSC799334; s2696; ZINC59224388; AKOS027250725; BCP9000717; CCG-269678; CS-0590; DB12180; GDC-0980.1; NSC-764091; NSC-799334; GDC-0980 - RG7422; NCGC00263109-03; NCGC00263109-13; (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperaz; AS-16289; HY-13246; SW219472-1; X7458; D10543; CAS:1032754-93-0;GDC-0980; G-038390; GDC-0980,CAS:1032754-93-0; J-502360; Q27074481; G-038390.1; (S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1 -one
• Indication:
  In total 2 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Phase 2; [1]
  Triple negative breast cancer [ICD-11: 2C60-2C6Y]; Phase 2; [1]
• Target: RAC-alpha serine/threonine-protein kinase (AKT1); AKT1_HUMAN; [1]
• Target: RAC-gamma serine/threonine-protein kinase (AKT3); AKT3_HUMAN; [1]
• Formula: 5
• IsoSMILES: CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)[C@H](C)O
• InChI: InChI=1S/C23H30N8O3S/c1-14-17(13-29-3-5-31(6-4-29)22(33)15(2)32)35-19-18(14)27-20(16-11-25-23(24)26-12-16)28-21(19)30-7-9-34-10-8-30/h11-12,15,32H,3-10,13H2,1-2H3,(H2,24,25,26)/t15-/m0/s1
• InChIKey: YOVVNQKCSKSHKT-HNNXBMFYSA-N
• PubChem CID: 25254071
• TTD Drug ID: D01ZAQ
• DrugBank ID: DB12180

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

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

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.E545K (c.1633G>A)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: DxS allele-specific PCR; qRT-PCR assays; Sanger sequencing assay
• Experiment for Drug Resistance: CTCAE assay

Pleural mesothelioma [ICD-11: 2C26]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.R88Q (c.263G>A)
• Sensitive Disease: Malignant pleural mesothelioma [ICD-11: 2C26.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: .; N.A.
• Experiment for Molecule Alteration: DxS allele-specific PCR; qRT-PCR assays; Sanger sequencing assay
• Experiment for Drug Resistance: CTCAE assay

Head and neck cancer [ICD-11: 2D42]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.E542K (c.1624G>A)
• Sensitive Disease: Head and neck squamous cell carcinoma [ICD-11: 2D42.1]
• Experimental Note: Identified from the Human Clinical Data
• Experiment for Molecule Alteration: DxS allele-specific PCR; qRT-PCR assays; Sanger sequencing assay
• Experiment for Drug Resistance: CTCAE assay

References

• Ref 1: Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid TumorsClin Cancer Res. 2016 Jun 15;22(12):2874-84. doi: 10.1158/1078-0432.CCR-15-2225. Epub 2016 Jan 19.