Drug intelligence / Profile preview

ethinyl estradiol + norethindrone acetate + orlistat + sibutramine

Development stage
Preclinical
Lead developer
Allergan
Modality
Small Molecules
Administration
Oral
01

Overview

This is a hypothetical or non-standard combination drug containing four active pharmaceutical ingredients: - **Ethinyl estradiol** (a synthetic estrogen) - **Norethindrone acetate** (a synthetic progestin) - **Orlistat** (a gastrointestinal lipase inhibitor for weight loss) - **Sibutramine** (a centrally acting serotonin-norepinephrine-dopamine reuptake inhibitor, formerly used for weight loss but withdrawn from many markets due to cardiovascular risk). Ethinyl estradiol and norethindrone acetate are commonly combined as oral contraceptives or hormone replacement therapy, working by inhibiting ovulation, altering cervical mucus, and modifying the endometrial lining[2][4][6]. Orlistat acts locally in the gut to inhibit fat absorption by blocking pancreatic and gastric lipases. Sibutramine increases satiety via inhibition of monoamine reuptake in the central nervous system[8]. There is no evidence that this four-drug combination exists as a marketed product; however, combinations of orlistat and sibutramine have been studied experimentally for obesity treatment[7].

02

Targets

NET (Norepinephrine Transporter)ER (Estrogen receptor)DAT (Dopamine plasma membrane transport protein)PNLIP (Pancreatic triacylglycerol lipase)SERT (Sodium-dependent serotonin transporter)LIPF (Gastric lipase)PR (Progesterone receptor)

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