FDA Approves NEXTSTELLIS Oral Contraceptive

April 16, 2021
Kenny Walter

Kenny Walter is an editor with HCPLive. Prior to joining MJH Life Sciences in 2019, he worked as a digital reporter covering nanotechnology, life sciences, material science and more with R&D Magazine. He graduated with a degree in journalism from Temple University in 2008 and began his career as a local reporter for a chain of weekly newspapers based on the Jersey shore. When not working, he enjoys going to the beach and enjoying the shore in the summer and watching North Carolina Tar Heel basketball in the winter.

The approval represents the first and only contraceptive pill containing E4, a natural occurring estrogen.

The US Food and Drug Administration (FDA) has approved 3 mg drospirenone [DRSP] and 14.2 mg estetrol [E4] tablets (NEXTSTELLIS) as an oral contraceptive.

The approval, awarded to Mayne Pharma, represents the first and only contraceptive pill containing E4, a natural occurring estrogen, now produced from a plant source. The substance has a unique mechanism of action that offers potential advantages over other estrogens.

The Product

E4 represents the first estrogen to that is a native estrogen with selective actions in tissues (NEST), with more selective activity in tissues, focusing on those needed to support contraceptive efficacy, cycle control and other beneficial effects of estrogen.

The product pairs with E4, which has a 24-28 hour half-life, with the proven progestin drospirenone, specifically chosen due to its long half-life (~30 hours) and its anti-androgenic and anti-ineralocorticoid properties.

Clinical Trials

The approval is based on a clinical study program that included a diverse patient population with women both starting and switching birth control, as well as patients with a body mass index (BMI) of up to 35 kg/m2.

There are nearly 10 million women in the US who use short-acting combination contraceptives, 99% of which contain ethinyl estradiol (EE), a synthetic estrogen that binds widely to all estrogen receptors in the body.

"When speaking with patients about their contraceptive options, one of the most common concerns is side effects," said Mitchell Creinin, Professor and Director of Family Planning at the University of California, Davis, in a statement. "NEXTSTELLIS is an innovative contraceptive that has been shown to be not only safe and effective, but also well tolerated in clinical trials with a desirable bleeding profile and minimal impact on triglycerides, cholesterol, and glucose, as well as weight and endocrine markers."