RO-5045337 (RG7112) is a small molecule that binds to a MDM2, a negative regulator of tumor-supressor protein p53. It was discovered by Roche and investigated in clinical trials against solid tumors, leukemias and sarcomas.

Revexepride is a selective 5-hydroxytryptamine receptor 4 agonist and member of a class of prokinetic agents that stimulate gastric emptying. Revexepride is thought to stimulate the release of acetylcholine at the myenteric plexus, leading to increased gastrointestinal contractions. This drug has been evaluated for potential use in treatment of gastroesophageal reflux disease. Phase I studies in healthy volunteers have shown no serious adverse events after administration of revexepride. However, a phase II study reported respiratory, thoracic and mediastinal disorders and pulmonary hypertension in 1 patient (0.85%). Furthermore, a European clinical trial showed that four weeks of treatment did not improve symptoms or gastric emptying in patients with symptoms suggestive of gastroparesis compared to placebo.

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

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.

INCB9471 is a non-competitive, potent and selective CCR5 small-molecule antagonist patented by pharmaceutical company Incyte Corporation for treatment of human immunodeficiency virus infection. INCB9471 potently inhibited macrophage inflammatory protein-1beta-induced monocyte migration and infection of peripheral blood mononuclear cells by a panel of R5-HIV-1 strains. INCB9471 was shown to be safe and highly efficacious in reducing HIV viral load in phase I and II human clinical trials

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.

Hexasonium, an anticholinergic agent, was studied as a spasmolytic. Information about the current use of this drug is not available.

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.