Drug Information

Drug (ID: DG00356) and It's Reported Resistant Information

• Name: S-1
• Synonyms: S-1; BMS 247616; S 1; S 1 (antitumor agent); TS 1; TS 1 (pharmaceutical)
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Lung cancer [ICD-11: 2C25]; [1]
• Formula: C17H19ClFKN6O9
• IsoSMILES: C1CC(OC1)N2CC(C(=O)NC2=O)F.C1C(=O)C(=CNC1=O)Cl.C1(NC(=O)NC(=O)N1)C(=O)[O-].[K+]
• InChI: 1S/C8H11FN2O3.C5H4ClNO2.C4H5N3O4.K/c9-5-4-11(6-2-1-3-14-6)8(13)10-7(5)12;6-3-2-7-5(9)1-4(3)8;8-2(9)1-5-3(10)7-4(11)6-1;/h5-6H,1-4H2,(H,10,12,13);2H,1H2,(H,7,9);1H,(H,8,9)(H3,5,6,7,10,11);/q;;;+1/p-1
• InChIKey: IOYPGLLFUCOOCZ-UHFFFAOYSA-M
• PubChem CID: 146157327

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Lung cancer [ICD-11: 2C25]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.T790M
• Resistant Disease: EGFR-mutant non-small cell lung cancer [ICD-11: 2C25.7]
• Experimental Note: Identified from the Human Clinical Data
• In Vivo Model: A retrospective survey in conducting clinical studies; Homo sapiens
• Experiment for Molecule Alteration: MGB SNP detection kit assay; Mutation Detection assay
• Experiment for Drug Resistance: Digital PCR assay
• Mechanism Description: Resistance mechanisms to EGFR-TkI therapy in EGFR-mutated NSCLC include secondary EGFR T790M mutation, c-Met amplification, PIk3CA mutation, and transformation to small-cell lung cancer.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Structural variation; Amplification
• Resistant Disease: EGFR-mutant non-small cell lung cancer [ICD-11: 2C25.7]
• Experimental Note: Identified from the Human Clinical Data
• In Vivo Model: A retrospective survey in conducting clinical studies; Homo sapiens
• Experiment for Molecule Alteration: MGB SNP detection kit assay; Mutation Detection assay
• Experiment for Drug Resistance: Digital PCR assay
• Mechanism Description: Resistance mechanisms to EGFR-TkI therapy in EGFR-mutated NSCLC include secondary EGFR T790M mutation, c-Met amplification, PIk3CA mutation, and transformation to small-cell lung cancer.

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

• Molecule Alteration: Mutation; .
• Resistant Disease: EGFR-mutant non-small cell lung cancer [ICD-11: 2C25.7]
• Experimental Note: Identified from the Human Clinical Data
• In Vivo Model: A retrospective survey in conducting clinical studies; Homo sapiens
• Experiment for Molecule Alteration: MGB SNP detection kit assay; Mutation Detection assay
• Experiment for Drug Resistance: Digital PCR assay
• Mechanism Description: Resistance mechanisms to EGFR-TkI therapy in EGFR-mutated NSCLC include secondary EGFR T790M mutation, c-Met amplification, PIk3CA mutation, and transformation to small-cell lung cancer.

References

• Ref 1: Noninvasive monitoring of the genetic evolution of EGFR-mutant non-small-cell lung cancer by analyzing circulating tumor DNA during combination chemotherapy with gefitinib and pemetrexed or S-1. Onco Targets Ther. 2016 Aug 24;9:5287-95. doi: 10.2147/OTT.S105976. eCollection 2016.