Drug intelligence / Profile preview

AP-22408

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
01

Overview

AP‐22408 is an experimental small molecule inhibitor targeting the proto-oncogene tyrosine-protein kinase Src (c-Src), a non-receptor tyrosine kinase implicated in cancer progression and bone homeostasis. It is a dual c-Src/Abl inhibitor that has demonstrated efficacy in preclinical models for reducing bone metastases. The compound belongs to the class of phenylalanine derivatives and contains phosphonic acid groups. Its primary research indications are osteoporosis and other bone-related diseases such as Paget's disease of bone, osteolytic bone metastasis from cancer (including skeletal metastases), and hypercalcemia associated with malignancy[1][4][6]. There are no approved clinical uses or ongoing clinical trials beyond preclinical studies.

Other names
268741-43-1Phosphonic acid, (4-((2S)-2-(acetylamino)-3-(((5S)-3-(aminocarbonyl)-2-(cyclohexylmethoxy)-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-yl)amino)-3-oxopropyl)-1,2-phenylene)bis-Phosphonic acid, P,P'-(4-((2S)-2-(acetylamino)-3–(((5S)–3–(aminocarbonyl)–2–(cyclohexylmethoxy)–6,7,8,9-tetrahydro–5H-benzocyclohepten–5‑yl)amino)‑3‑oxopropyl)‑1,2‑phenylene)bis-
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)

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