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capecitabine + perifosine
- Development stage
- Unknown
- Lead developer
- Akebia Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Capecitabine + perifosine is an investigational oral combination therapy for cancer, primarily studied in metastatic colorectal cancer (mCRC). Capecitabine is a prodrug of 5-fluorouracil (5-FU), an antimetabolite that inhibits DNA synthesis by interfering with thymidylate synthase. Perifosine is a synthetic alkylphospholipid that modulates multiple signal transduction pathways, notably inhibiting Akt activation in the phosphoinositide 3-kinase (PI3K) pathway, as well as affecting MAPK and JNK pathways. Perifosine also inhibits NF-κB and blocks localization of Akt to the cell membrane, promoting apoptosis and potentially overcoming resistance to chemotherapy. The combination has demonstrated synergistic effects in preclinical and clinical studies, showing improved time to progression and overall survival compared to capecitabine alone in patients with refractory mCRC[1][2][4][5][6].
- Brand names
- Xeloda
- Other names
- P-CAP
02
Targets
AKT (RAC-alpha serine/threonine-protein kinase)TS (Thymidylate synthase)
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