Mapracorat (BAY-865319, BOL-303242-X or ZK-245186) is a selective non-steroid glucocorticoid receptor agonist exerting anti-inflammatory activity. Mapracorat showed partial attenuation of the classical NF-κB pathway, consistent with traditional steroids. However, mapracorat uniquely potentiated a novel anti-inflammatory mechanism through rapid upregulation of RelB, an anti-inflammatory member of the NF-κB alternative pathway. Mapracorat was being studied in the treatment of ocular and skin inflammatory diseases.

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.

Gadopenamide is an MRI contrast agent that was introduced in 1991. It has been investigated as a potential clinical contrast medium by Schering AG (Germany), but has never been used as such.

Nocloprost is a stable prostaglandin E2 analog with gastroprotective and ulcer-healing properties. It shows very high gastroprotective potency, relatively weak gastric inhibitory activity, and low systemic bioavailability after oral administration. Schering AG have discontinued development of the drug, which was in phase II clinical trials for the treatment of peptic ulcer.

Vilaprisan, a small molecule progesterone receptor antagonist is being developed by Bayer HealthCare Pharmaceuticals (formerly Bayer Schering Pharma) for the treatment of endometriosis and uterine leiomyoma. Hormonal imbalance observed in women with endometriosis is a potential target for treating endometriosis. Vilaprisan is a highly selective steroidal progesterone receptor modulator (SPRM). It is a partial agonist of progesterone receptor, which means that the drug activates progesterone receptors to a certain degree upon binding. This triggers a cascade of biochemical reactions that result in the suppression of prostaglandin production. This, in turn, relieves symptoms such as pain and bleeding. Modulating progesterone by taking vilaprisan might help in treating endometriosis over the long term. Phase I and II studies give encouraging results on the efficacy of vilaprisan at different doses. Like other SPRMs, vilaprisan induces benign changes of endometrium (PR modulator-associated endometrial changes, PAECs). These disappear as treatment is discontinued. Unlike GnRHa treatment, neither UPA nor vilaprisan induce hypoestrogenism and associated symptoms. Phase III studies are ongoing to confirm efficacy and safety of vilaprisan in long-term treatment of symptomatic fibroids.

Roniciclib (BAY1000394) is a pan-cyclin-dependent kinase inhibitor that has been developed for treatment in small cell lung carcinoma and solid tumors. Roniciclib targets certain key proteins that are essential for the survival of cancer cells, resulting in decreased tumor growth. Phase I studies to evaluate the safety, tolerability and pharmacokinetics of roniciclib have been completed successfully. In phase II studies, roniciclib was found to be well tolerated and showed promising efficacy when combined with chemotherapy in small cell lung carcinoma patients. However, due to an observed safety signal (treatment-emergent adverse events) in one phase II study, other clinical trials have been discontinued and further development of roniciclib was terminated.

Anxiolytic drug, Gedocarnil [SH 530, ZK 113315], was undergoing phase I clinical trials with Schering AG in Germany as a potential nootropic agent. However it`s development for the treatment of cognition disorders was discontinued.

Flosulide, a selective cyclooxygenase-2 (COX-2) inhibitor, was studied for the treatment for inflammatory diseases. It was shown, that selective inhibition of COX-2 could alter renal function and could be useful in the therapy of esophageal cancer. Experiments on rodent have revealed that therapeutic use of flosulide in proteinuria could be a benefit.

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.