Drug intelligence / Profile preview

APG-2449 + pegylated liposomal doxorubicin

Development stage
Unknown
Lead developer
Ascentage Pharma
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Oral, Intravenous
01

Overview

APG-2449 + pegylated liposomal doxorubicin is an experimental combination therapy currently under investigation for cancer treatment. APG-2449 is a small molecule, orally active, third-generation, multitargeted tyrosine kinase inhibitor that inhibits focal adhesion kinase (FAK), anaplastic lymphoma kinase (ALK), and ROS proto-oncogene 1 receptor tyrosine kinase (ROS1), as well as other kinases such as IGF1R, LRRK2, and LTK[1][3][4]. Pegylated liposomal doxorubicin is a liposome-encapsulated formulation of doxorubicin, an anthracycline chemotherapy agent that inhibits topoisomerase II, thereby blocking DNA replication and cancer cell proliferation. The pegylated liposomal formulation is engineered to remain in the bloodstream longer, allowing more of the drug to reach tumors and reducing exposure to healthy tissue[2][5]. The combination is mainly being studied in advanced solid tumors, including ovarian cancer and non-small cell lung cancer (NSCLC), aiming to overcome resistance mechanisms and improve anticancer efficacy[3][4][6].

Other names
doxorubicin hydrochloride liposomepegylated doxorubicinpegylated liposomal doxorubicin
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)TOP2A (DNA topoisomerase II)DNAROS1 (Proto-oncogene tyrosine-protein kinase ROS)

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