befotertinib   Click here for help

GtoPdb Ligand ID: 12951

Synonyms: compound 4 [WO2019218987A1] [2] | D-0316 | D0316 | Surmana®
Approved drug
befotertinib is an approved drug (China NMPA (2023))
Compound class: Synthetic organic
Comment: Befotertinib (D-0316) is an third generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that was developed as a treatment for non-small cell lung cancer (NSCLC) [2].
2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 9
Hydrogen bond donors 2
Rotatable bonds 13
Topological polar surface area 84.8
Molecular weight 567.61
XLogP 3.32
No. Lipinski's rules broken 2
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Canonical SMILES C=CC(=O)NC1=C(C=C(C(=C1)NC2=NC=CC(=N2)C3=CN(CC(F)(F)F)C4=C3C=CC=C4)OC)N(C)CCN(C)C
InChI InChI=1S/C29H32F3N7O2/c1-6-27(40)34-22-15-23(26(41-5)16-25(22)38(4)14-13-37(2)3)36-28-33-12-11-21(35-28)20-17-39(18-29(30,31)32)24-10-8-7-9-19(20)24/h6-12,15-17H,1,13-14,18H2,2-5H3,(H,34,40)(H,33,35,36)
1. Blair HA. (2023)
Befotertinib: First Approval.
Drugs, 83 (15): 1433-1437. [PMID:37751131]
2. Dai X, Jiang Y. (2019)
Egfr inhibitors.
Patent number: WO2019218987A1. Assignee: Inventisbio Shanghai Ltd.. Priority date: 14/05/2019. Publication date: 21/11/2019.
3. Jiang Y. (2015)
Pyrimidine or pyridine compound, and preparation method and pharmaceutical application thereof.
Patent number: CN105085489A. Assignee: Yifang Biotechnology (Shanghai) Co.,Ltd.; Betta Pharmaceuticals Co Ltd. Priority date: 01/04/2015. Publication date: 25/11/2015.
4. Lu S, Zhang Y, Zhang G, Zhou J, Cang S, Cheng Y, Wu G, Cao P, Lv D, Jian H et al.. (2022)
Efficacy and Safety of Befotertinib (D-0316) in Patients With EGFR T790M-Mutated NSCLC That Had Progressed After Prior EGFR Tyrosine Kinase Inhibitor Therapy: A Phase 2, Multicenter, Single-Arm, Open-Label Study.
J Thorac Oncol, 17 (10): 1192-1204. [PMID:35724798]
5. Lu S, Zhou J, Jian H, Wu L, Cheng Y, Fan Y, Fang J, Chen G, Zhang Z, Lv D et al.. (2023)
Befotertinib (D-0316) versus icotinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer: a multicentre, open-label, randomised phase 3 study.
Lancet Respir Med, 11 (10): 905-915. [PMID:37244266]