Drug intelligence / Profile preview

pregabalin + PF-00489791

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Combination of **pregabalin** (a well-established alpha-2-delta ligand approved for neuropathic pain) and **PF-00489791** (an experimental phosphodiesterase 5A (PDE5A) inhibitor initially developed by Pfizer). This combination was investigated in clinical trials for improved analgesic efficacy in post-herpetic neuralgia, a chronic neuropathic pain condition. Pregabalin reduces neuronal excitability by inhibiting voltage-gated calcium channels, while PF-00489791 acts via a distinct mechanism by inhibiting PDE5A, likely modulating cyclic GMP signaling and influencing pain pathways[8][9]. The combination was expected to provide enhanced pain control compared to pregabalin monotherapy[4][5][6].

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)

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