Dimesone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic activity.

Nifuratrone is a nitrofuran which was used for the control of Salmonella choleraesuis in swine. It was also used for the treatment of gonorrhea.

Gestaclone was developed as a progesterone receptor agonist; however, this compound has never been marketed. Information about the current use of this compound is not available.

1H-2-BENZOPYRAN-3-ACETIC ACID, 8-HYDROXY-6-METHOXY-Α-METHYL-1-OXO- (NM-3) is an orally bioavailable antiangiogenic isocoumarin with potential antineoplastic activity. NM-3 inhibits vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor, thereby inhibiting endothelial cell proliferation. NM-3 induces apoptosis by a mechanism involving reactive oxygen species. In human MCF-7 and ZR-75-1 breast cancer cells, NM-3 induces the p21 cyclin-dependent kinase inhibitor, cell cycle arrest at G1-S-phase, and necrotic cell death. NM-3 has been used in trials studying the treatment of solid tumours.

HSD-016 was discovered as an orally efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of diabetes. The phase I in clinical trials for the drug was completed; however, information about further studies is not available.

Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.

NPV-LEQ506 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. NPV-LEQ506 selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway, thereby inhibiting tumor cell growth. NPV-LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. NPV-LEQ506 has been in clinical trials with Novartis studying the treatment of advanced solid tumors, recurrent or refractory medulloblastoma, and locally advanced or metastatic basal cell carcinoma.

Foxy-5, a wingless-type mammary tumor virus integration site 5A (WNT5A)-mimicking peptide, was studied for the treatment of cancer. Foxy-5 is participating in phase II clinical trial as neo-adjuvant therapy for the treatment of patients with wnt-5a low colon cancer. Besides, Foxy-5 was used in phase I clinical trial, for the treatment of prostate cancer patients with tumors exhibiting absent or low WNT5A expression.