Andamertinib

Andamertinib
Clinical data
Other names	GTPL13732, PLB1004
Identifiers
	IUPAC name N-[4-Methoxy-2-[4-(3-methoxyazetidin-1-yl)piperidin-1-yl]-5-[[6-(1-methylindazol-5-yl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide;
CAS Number	2254145-43-0;
PubChem CID	146498390;
IUPHAR/BPS	13732;
UNII	5X3KAG7ZBW;
Chemical and physical data
Formula	C31H36N8O3
Molar mass	568.682 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C2=C(C=C(C=C2)C3=CC(=NC=N3)NC4=C(C=C(C(=C4)NC(=O)C=C)N5CCC(CC5)N6CC(C6)OC)OC)C=N1;
	InChI InChI=1S/C31H36N8O3/c1-5-31(40)36-25-13-26(29(42-4)15-28(25)38-10-8-22(9-11-38)39-17-23(18-39)41-3)35-30-14-24(32-19-33-30)20-6-7-27-21(12-20)16-34-37(27)2/h5-7,12-16,19,22-23H,1,8-11,17-18H2,2-4H3,(H,36,40)(H,32,33,35); Key:KKPCZGCBAIJCOU-UHFFFAOYSA-N;

Andamertinib is an investigational new drug that is being develop by Avistone Biotechnology Co., Ltd. for the treatment of non-small-cell lung cancer (NSCLC). It is an epidermal growth factor receptor (EGFR) antagonist.^[1]^[2]^[3]

Andamertinib is an irreversible EGFR inhibitor designed to target EGFR with exon 20 insertion mutations.^[4]

Clinical trials

The following clinical trials are evaluating andamertinib for treating NSCLC:

phase 2 (on going)^[5]
phase 2 (on going) in combination wth vebreltinib or osimertinib^[6]
phase 3 (recruiting) in combination with vebreltinib or pemetrexed plus carboplatin or cisplatin^[7]

↑ Yang JJ, Mu Y, Wang ZH, Duan JC, Zhang Y, Wu L, et al. (March 2026). "Andamertinib in Advanced NSCLC With EGFR Exon 20 Insertions After Platinum-Based Chemotherapy or Immunotherapy: Results From the Phase 2 KANNON Study". Journal of Thoracic Oncology. 21 (3): 103518. doi:10.1016/j.jtho.2025.11.008. PMID 41248848.
↑ Zhao J, Xu W, Zhou F, Zhang X, Zhou M, Miao D, et al. (January 2026). "Navigating the landscape of EGFR TKI resistance in EGFR-mutant NSCLC - mechanisms and evolving treatment approaches". Nature Reviews. Clinical Oncology. 23 (1): 63–83. doi:10.1038/s41571-025-01085-z. PMID 41219394.
↑ "Andamertinib - Avistone Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
↑ "Andamertinib | Ligand page". IUPHAR/BPS Guide to PHARMACOLOGY.
↑ Clinical trial number NCT07336732 for "Andamertinib With or Without Platinum-doublet Chemotherapy Versus Platinum-doublet Chemotherapy in Patients With NSCLC Harboring Atypical EGFR Mutations" at ClinicalTrials.gov
↑ Clinical trial number NCT06574347 for "Vebreltinib Plus PLB1004 as the First-line Therapy for Patients With EGFRm+/MET+ Locally Advanced or Metastatic NSCLC." at ClinicalTrials.gov
↑ Clinical trial number NCT06970782 for "Vebreltinib Plus PLB1004 Versus Platinum-based Doublet Chemotherapy in Patients With EGFRm, MET+, Locally Advanced or Metastatic NSCLC Following EGFR-TKI Failure" at ClinicalTrials.gov