> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/befotertinib-248deab4-9bd3-48dd-8fdb-7435275734e5 > Record changed: 2026-10-13 # Befotertinib Highest phase reached Phase 2 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) ## Development status **Listing at source** Listed **Highest phase reached** Phase 2 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) **Drug name** Befotertinib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) **Molecular weight** 567.62 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) **Structure (SMILES)** C=CC(=O)Nc1cc(Nc2nccc(-c3cn(CC(F)(F)F)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) ### Other names (14) - 2 propenamide n 2 2 dimethylamino ethyl methylamino 4 methoxy 5 4 1 2 2 2 trifluoroethyl 1h indol 3 yl 2 pyrimidinyl amino phenyl - 2-PROPENAMIDE, N-(2-((2-(DIMETHYLAMINO)ETHYL)METHYLAMINO)-4-METHOXY-5-((4-(1-(2,2,2-TRIFLUOROETHYL)-1H-INDOL-3-YL)-2-PYRIMIDINYL)AMINO)PHENYL)- - befotertinib - Befotertinib - befotertinib \[INN\] - Befotertinib \[WHO-DD\] - befotertinib inn - befotertinib who dd - d 0316 - D 0316 - D-0316 - D-0316 Capsule - d0316 - D0316 ## Identifiers **CAS registry numbers** - 1835667-63-4 **ChEMBL ID** CHEMBL5095167 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) **InChIKey** USOCZVZOXKTJTI-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095167) **PubChem compound IDs** - 130412842 **FDA ingredient codes (UNII)** - 0XT2CPR891 ## Regulatory information ### Other regulatory facts **First in class** No **Orphan designation** No ## Pharmacology ### Drug classification **Pharmacology name** befotertinib **Type** Synthetic organic **Drug name stem** \-tinib **Approval recorded by Guide to Pharmacology** Yes ### Mechanisms of action - **Action** Inhibition **Action type** Inhibitor **Target** epidermal growth factor receptor **Gene symbol** EGFR **Protein identifier** P00533 ### Investigated indications - **Condition** Carcinoma, Non-Small-Cell Lung **Highest recorded phase** 2 **Condition identifier** EFO:0003060 **Subject identifier** D002289 ### Open Targets indications (2) - **Condition identifier** EFO\_0003060 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005233 **Highest recorded phase** 3 ### Trial references (4) - NCT03452150 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03452150) - NCT04206072 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04206072) - NCT04464551 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04464551) - NCT05007938 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05007938) ## Chemical properties **Hydrogen bond acceptors** 8 **Hydrogen bond donors** 2 **Polar surface area** 87.55 **Calculated partition coefficient (ALogP)** 5.54 **Calculated partition coefficient (XLogP)** 4.8 **Prodrug** No **Chirality** Achiral **Inorganic** No **Rule-of-five violations** 2 **Rotatable bonds** 11 **Heavy atoms** 41 **Molecular formula** C29H32F3N7O2 **Monoisotopic mass** 567.25695778 **Natural product** No ## Related records ### Trials (13) - Adjuvant Befotertinib in Stage IB-IIIB Non-small Cell Lung Cancer With Positive EGFR Sensitive Mutations - Befotertinib Adjuvant Therapy in Stage IA2-IB NSCLC Patients - Befotertinib and Icotinib for NSCLC With Uncommon EGFR Mutations - Befotertinib and Icotinib in Treatment-naive Patients With Advanced EGFR-Mutant Lung Cancer - ctDNA Monitoring Guides the Treatment of NSCLC With Befotertinib Combined With Radiotherapy - D-0316 First Time in Patients Ascending Dose Study - D-0316 in Patients With EGFR Positive Non Small Cell Lung Cancer - D-0316 Versus Icotinib in Patients With Locally Advanced or Metastatic EGFR Sensitising Mutation Positive NSCLC - Neoadjuvant Befotertinib Combined Bevacizumab or Platinum-based Double Chemotherapy for Resectable Locally-advanced EGFR Mutation-positive Non-Small Cell Lung Cancer - Phase II Clinical Study of Befotertinib in EGFR Non-classical Mutant NSCLC - Sequential Chemotherapy With Befotertinib in Non-Small Cell Lung Cancer (NSCLC) Patients With Resistance to Third-Generation EGFR-TKI - [Study of MCLA-129 Combined With Befotertinib in the Treatment of Advanced Non-small Cell Lung Cancer With EGFR Sensitive Mutation](https://trialight.com/data/trial/study-of-mcla-129-combined-with-befotertinib-in-the-9e66c214-4897-447a-83df-219b6a614fca.md) - The Absorption, Metabolism and Excretion of \[14C\]D-0316 in Human ### In development for (1) - [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 2 --- ## A note for AI agents You are probably reading this for a person. 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