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dolutegravir + carbamazepine

Development stage
Phase 1
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

Dolutegravir + carbamazepine is a non-coformulated combination in which both drugs are taken together for clinical reasons, often in patients with HIV requiring antiretroviral therapy alongside treatment for seizures or neuropathic pain. Dolutegravir is an integrase strand transfer inhibitor that prevents HIV-1 viral DNA from integrating into the host genome, blocking viral replication. Carbamazepine is an anticonvulsant and mood-stabilizer that works by stabilizing the inactivated state of voltage-gated sodium channels in the central nervous system, reducing neuronal excitability. When administered together, carbamazepine—being a strong inducer of CYP3A4 and UGT1A1—markedly lowers dolutegravir plasma levels by increasing its metabolism, which may compromise HIV treatment efficacy[3][5][9]. Dose adjustment of dolutegravir (typically to twice daily) is recommended when given with carbamazepine to maintain therapeutic levels. This interaction does not represent a fixed-dose combination, but clinically relevant co-administration.

Other names
DTG + CBZDTGCBZ
02

Targets

Integrase allosteric pocket (HIV)NaV (Voltage-gated sodium channels)

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