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Drug intelligence / Profile preview
PH-797804 + erythromycin
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PH-797804 is a potent, selective, ATP-competitive small molecule inhibitor of p38α mitogen-activated protein kinase (MAPK), originally developed by Pfizer for the treatment of inflammatory conditions such as chronic obstructive pulmonary disease (COPD) and rheumatoid arthritis. Erythromycin is a macrolide antibiotic that also functions as a potent mechanism-based inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. The combination of PH-797804 and erythromycin has been specifically utilized in clinical pharmacology studies to evaluate drug-drug interaction (DDI) profiles. Specifically, these studies aimed to determine how the inhibition of CYP3A4 by erythromycin affects the systemic exposure and pharmacokinetics of PH-797804, which is a substrate for the CYP3A4 metabolic pathway. Clinical development of PH-797804 was ultimately discontinued by Pfizer.
- Other names
- PH-797804 and erythromycinPH797804 and erythromycinPH 797804 and erythromycin
02
Targets
Bacterial 50S ribosomal subunitRK (Ribokinase)MAPK11 (p38 beta mitogen-activated protein kinase)CYP3A4 (Cytochrome P450 3A4)MAPK14 (p38 mitogen-activated protein kinase alpha)
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