Drug Information

Drug (ID: DG00071) and It's Reported Resistant Information

Name	Olmutinib
Indication	In total 1 Indication(s) Lung cancer [ICD-11: 2C25] Approved [1]
Structure
Drug Resistance Disease(s)	Disease(s) with Clinically Reported Resistance for This Drug (1 diseases) Lung cancer [ICD-11: 2C25] [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	C26H26N6O2S
IsoSMILES	CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4
InChI	1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)
InChIKey	FDMQDKQUTRLUBU-UHFFFAOYSA-N
PubChem CID	54758501
TTD Drug ID	D05NUH
DrugBank ID	DB13164

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

Click to Show/Hide the Resistance Disease of This Class

Lung cancer [ICD-11: 2C25]

Click to Show/Hide

Drug Resistance Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)		Click to Show/Hide
Key Molecule: Epidermal growth factor receptor (EGFR)			[1]
Molecule Alteration	Missense mutation	p.C797S	Molecule Info
Resistant Disease	Lung adenocarcinoma [ICD-11: 2C25.0]		Disease Info
Experimental Note	Identified from the Human Clinical Data
Experiment for Molecule Alteration	Next-generation sequencing assay
Experiment for Drug Resistance	Computed tomography assay; Progression-free survival assay
Mechanism Description	A recent preclinical study reported that EGFR C797S, L718Q, and L844V mutations cause resistance to both WZ4002 and CO-1686 but only EGFR C797S leads to AZD9291 resistance, suggesting that C797S can serve as acquired resistance to irreversible pyrimidine-based EGFR inhibitors given the similar chemical structure of third-generation EGFR TkIs.

References

Ref 1	Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non-Small Cell Lung Cancer. J Thorac Oncol. 2016 Apr;11(4):e45-7. doi: 10.1016/j.jtho.2015.12.093. Epub 2015 Dec 31.