(+)-Fadrozole (FAD-286) is an aldosterone synthase inhibitor. The drug was tested in vivo in preclinical models of hypertension, heart failure and was shown to reduce retinal neovascularization in rats with oxygen-induced retinopathy.

AT-406 (DEBIO-1143, SM-406), is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). AT-406 inhibits cancer cell growth in various human cancer cell lines. It has good oral bioavailability in mice, rats, non-human primates, and dogs, is highly effective in induction of apoptosis in xenograft tumors, and is capable of complete inhibition of tumor growth. Debiopharm under a licence from Ascenta Therapeutics is developing AT-406 for the treatment of cancers.

Monophosphothiamine is thiamine derivative used for the treatment of neuritis, polyneuritis, asthenic conditions (weakness), as an additional remedy for chronic blood circulation insufficiency, chronic gastritis accompanied by motor and secretory disorders functions of the stomach. Monophosphothiamine underwent metabolic phosphorylation to active metabolite thiamine pyrophosphate, that acts as a coenzyme in the different metabolic process.

CX-5461 represents an innovative-targeted agent with numerous differentiating features when compared to current options for treatment of hematologic cancers. CX-5461 is a first-in-class small molecule inhibitor of RNA polymerase I (Pol I) that triggers the nucleolar stress surveillance pathways to activate p53, without causing direct DNA damage. Molecular studies demonstrate that CX-5461 inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy, but not apoptosis, through a p53-independent process in solid tumor cell lines. Currently, CX-5461 is in clinical trial for patients with advanced hematological malignancies.

Mevastatin (compactin or ML-236B) is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This drug induces apoptosis and arrest of cancer cells in G1 phase. Therapeutic effects of mevastatin on serum level of lipoproteins and unbiquinone-10 in patients with familial hypercholesterolemia were investigated. However, that study was discontinued. In addition, mevastatin was investigated for the treatment of melanoma. It was suggested, that mevastatin was unlikely to prevent melanoma at standard doses. However, higher doses could have a role to play in adjuvant therapy by inhibiting growth and invasion of melanoma cells. Also was revealed, that mevastatin increased histone deacetylase inhibitor, LBH589-induced cell death in triple-negative breast cancer (TNBC) cells.