PF-06655075

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[(3R)-3-[[4-(4-methylpiperazin-1-yl)phenyl]amino]-3-oxopropyl]phenyl]amino]-3-phenylpropanoic acid | image = | width = | alt = | CAS_number = 1628835-09-4 | PubChem = 71587812 | ChemSpiderID = 32700000 | UNII = | KEGG = | ChEMBL = 3545115 | C=28 | H=32 | N=4 | O=3 | smiles = | InChI = | InChIKey = }}

PF-06655075 is an investigational drug developed by Pfizer for the treatment of various types of cancer. It is a small molecule inhibitor that targets specific proteins involved in the proliferation and survival of cancer cells.

Mechanism of Action

PF-06655075 functions as a selective inhibitor of the Bromodomain and Extra-Terminal motif (BET) family of proteins. BET proteins, such as BRD2, BRD3, and BRD4, are epigenetic "readers" that recognize acetylated lysine residues on histone tails, thereby regulating gene expression. By inhibiting BET proteins, PF-06655075 disrupts the transcription of oncogenes and other genes critical for cancer cell growth and survival.

Pharmacokinetics

The pharmacokinetic profile of PF-06655075 has been characterized in preclinical studies. It exhibits favorable oral bioavailability and a half-life that supports once-daily dosing. The drug is metabolized primarily in the liver and excreted via the renal and fecal routes.

Clinical Trials

PF-06655075 has undergone several phases of clinical trials to evaluate its safety, tolerability, and efficacy in patients with advanced solid tumors and hematological malignancies. Early-phase trials have demonstrated promising antitumor activity, particularly in cancers with specific genetic alterations that make them susceptible to BET inhibition.

Adverse Effects

Common adverse effects observed in clinical trials include fatigue, nausea, diarrhea, and hematological toxicities such as thrombocytopenia and anemia. These side effects are generally manageable with supportive care and dose adjustments.

Research and Development

Research on PF-06655075 is ongoing, with studies focusing on its use in combination with other anticancer agents, as well as its potential role in overcoming resistance to existing therapies. The drug's ability to modulate the immune response is also being explored, as BET inhibitors may enhance the efficacy of immunotherapy in certain cancer types.

Also see

• Bromodomain and Extra-Terminal motif
• Epigenetic therapy
• Cancer treatment
• Oncogene
• Immunotherapy