They also noted that the company by then had settled 1,977 cases for US$402.6 million, for an average of US$212,000 per case, while setting aside US$610.5 million to settle the others.As of July 17, 2015, there have been at least 4,000 lawsuits and claims still pending regarding VTE related to drospirenone. This is in addition to around 10,000 claims that Bayer has already settled without admitting liability. These claims of VTE have amounted to US$1.97 billion. Bayer also reached a settlement for arterial thromboembolic events, including stroke and heart attacks, for US$56.9 million. Research
A combination of ethinylestradiol, drospirenone, and prasterone is under development by Pantarhei Bioscience as a combined birth control pill for prevention of pregnancy in women. It includes prasterone (dehydroepiandrosterone; DHEA), an oral androgen prohormone, to replace testosterone and avoid testosterone deficiency caused by suppression of testosterone by ethinylestradiol and drospirenone. As of August 2018, the formulation is in phase II/III clinical trials.Drospirenone has been suggested for potential use as a progestin in male hormonal contraception.Drospirenone has been studied in forms for parenteral administration. References
Further reading
Archer DF (February 2007). "Drospirenone and estradiol: a new option for the postmenopausal woman". Climacteric. 10 Suppl 1: 3–10. doi:10.1080/13697130601114859. PMID 17364592. S2CID 9221524. Archer DF (February 2007). "Drospirenone-containing hormone therapy for postmenopausal women. Perspective on current data". J Reprod Med. 52 (2 Suppl): 159–64. PMID 17477110. Archer DF (2007). "Drospirenone, a progestin with added value for hypertensive postmenopausal women". Menopause. 14 (3 Pt 1): 352–4. doi:10.1097/gme.0b013e31804d440b. PMID 17414576. Batur P, Casey PM (February 2017).
It has about 100 to 500% of the affinity of aldosterone for the MR and about 50 to 230% of the affinity of progesterone for the MR. Drospirenone is about 5.5 to 11 times more potent as an antimineralocorticoid than spironolactone in animals. Accordingly, 3 to 4 mg drospirenone is said to be equivalent to about 20 to 25 mg spironolactone in terms of antimineralocorticoid activity. It has been said that the pharmacological profile of drospirenone more closely resembles that of progesterone than other progestins due to its antimineralocorticoid activity. Drospirenone is the only clinically used progestogen with prominent antimineralocorticoid activity besides progesterone. For comparison to progesterone, a 200 mg dose of oral progesterone is considered to be approximately equivalent in antimineralocorticoid effect to a 25 to 50 mg dose of spironolactone. Both drospirenone and progesterone are actually weak partial agonists of the MR in the absence of mineralocorticoids.Due to its antimineralocorticoid activity, drospirenone increases natriuresis, decreases water retention and blood pressure, and produces compensatory increases in plasma renin activity as well as circulating levels and urinary excretion of aldosterone. This has been shown to occur at doses of 2 to 4 mg/day. Similar effects occur during the luteal phase of the menstrual cycle due to increased progesterone levels and the resulting antagonism of the MR. Estrogens, particularly ethinylestradiol, activate liver production of angiotensinogen and increase levels of angiotensinogen and angiotensin II, thereby activating the renin–angiotensin–aldosterone system.