Drug intelligence / Profile preview

GSK2248761 + drospirenone + ethinyl estradiol

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

Overview

GSK2248761 + drospirenone + ethinyl estradiol is an investigational combination of a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with a combined oral contraceptive (COC) containing drospirenone (a progestin) and ethinyl estradiol (an estrogen). **GSK2248761** (fosdevirine) inhibits HIV-1 replication by binding directly to reverse transcriptase and blocking RNA/DNA-dependent DNA polymerase activities required for viral replication[1][3]. Drospirenone + ethinyl estradiol act by inhibiting ovulation, altering cervical mucus, and modifying endometrial lining to prevent pregnancy[4]. This combination has been studied for drug-drug interaction potential between HIV treatment and hormonal contraception. PK interaction studies show marginal increases in drospirenone exposure (∼18–22%) and no change in ethinyl estradiol, with no clinical need for contraceptive dose modification[1][3]. GSK2248761’s clinical development is currently on hold due to seizure risk identified in phase IIb HIV trials[1][3].

Brand names
No unique brand name for the combination
Other names
No unique other names for the triple combination
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseER (Estrogen receptor)PR (Progesterone receptor)

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