Phenovalin is the laxative agent.

Fluorfenidine F-18 is a radionucleotide used in positron emission tomography (PET) imaging procedures.

GET-73 (N-[(4-trifluoromethyl)benzyl]4-methoxybutyramide) is a compound with a structure related to that of gamma-hydroxybutyric acid (GHB), which is used in the treatment of alcohol withdrawal. Like GHB, GET-73 has the capacity to reduce alcohol intake in rats. GET-73 also exerts anxiolytic effects in rats and seemed to improve memory in a water maze test. Although the exact mechanism of GET-73 action is still unknown, it was suggested that an allosteric modulation of metabotropic glutamate receptor 5 (mGlu5 receptor) by GET-73 may represent the mechanism underlying the effects of the compound. GET73 was suggested to have a multifaceted pharmacological profile, importantly including the capacity to reduce alcohol drinking and anxiety-related behaviors. A phase II study was completed in November 2018, in which physical effects and changes in cognitive performance as a result of GET-73 administration were studied in alcohol-dependent individuals.

COH-29 is an antimetabolite drug developed at City of Hope Cancer Center. Compound targets human ribonucleotide reductase, a key enzyme in the deoxyribonucleotide biosynthesis. In preclinical studies, COH-29 induced double-strand breaks in BRCA1-defective breast cancer cells and has been shown to reduce tumor growth in leukemia and ovarian cancer models. In 2015, COH-29 was licensed to a biotech company Novonco. The drug is being evaluated in phase 1 clinical trial for the treatment of patients with solid tumors.

Amcasertib is an orally administered investigational agent designed to inhibit cancer stemness pathways, including Nanog, by targeting stemness kinases. Amcasertib is undergoing multiple Phase I and Phase II studies as monotherapy and combination therapy for treating a range of tumor types.

Voruciclib (also known as P1446A-05) is a flavone-based, potent and selective CDK 4/6 inhibitor with activity in multiple BRAF-mutant and wild type cell lines. It is currently in clinical trials in combination with BRAF inhibitor (PLX4032) to treat advanced BRAF-mutant melanoma. Voruciclib has significant inhibitory activity against cutaneous and uveal melanoma. Mechanistic studies revealed that P1446A-05 inhibits phosphorylation targets of CDK members, and induces cell cycle arrest and apoptosis irrespective of melanoma genotype or phenotype. Voruciclib Hydrochloride is in phase I clinical trials by Piramal Life Sciences for the treatment of chronic lymphocytic leukaemia and malignant melanoma.

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.

PAC-14028 was developed as a transient receptor potential vanilloid type 1 (TRPV1) antagonist. It is known that TRPV1 might be deeply associated with skin permeability barrier function, suggesting that modulation of TRPV1 might be beneficial for the skin disorders with barrier damages. Amorepacific developed a topical cream formulation of PAC-14028. This drug completed phase III clinical trial for the treatment of atopic dermatitis. In addition, PAC-14028 participated in phase II clinical trials to evaluate its safety and efficacy in seborrheic dermatitis and in rosacea. Moreover, PAC-14028 has been used in trials studying the treatment of pruritus.

MK-0249 is a potent H3 receptor inverse agonist patented by Abbott Laboratories for treatment of cognitive deficits. MK-0249 demonstrates promising results in preclinical models of cognitive disorders. MK0249 has been used in trials studying the treatment of Hypopnea Syndrome, Alzheimer's Disease, Paranoid Schizophrenia ets. Unfortunately, MK-0249 failed to demonstrate efficacy in schizophrenia, mild-to-moderate Alzheimer's Disease, attention-deficit/hyperactivity disorder, and future development has been discontinued.