MK-0773 is an orally active selective androgen receptor modulator. The safety and efficacy of MK-0773 was evaluated in sarcopenic elderly women. The MK-0773- induced improvements in lean body mass were not accompanied by statistically significant improvements in physical function. Higher dose of MK-0773 or longer duration of therapy might have resulted in improvements in physical function, but liver transaminase elevations likely preclude further development of MK-0773. Drug-candidate had been in phase I clinical trials for the treatment of osteoporosis.

Bizelesin (previously known as U-77779 or NSC 615291), a cyclopropylpyrroloindole antitumor agent acts as a bifunctional alkylating agent and produces DNA interstrand cross-links. This drug participated in phase I clinical trials in patients with advanced solid malignancies, however further development was discontinued.

Acridorex (BS 7573a) is an anorectic agent.

JNJ-872 is an inhibitor of influenza virus replication that offers a potential for the treatment of pandemic and seasonal influenza.

RO4929097 (R-4733) is a small-molecule inhibitor of gamma-secretase (γ-secretase) with high oral bioavailability leading to the blockade of Notch signaling in tumor cells. This compound was co-developed by Roche and National Cancer Institute (NCI). RO4929097 had been in phase II clinical trials for the treatment of melanoma, colorectal cancer, and pancreatic cancer. However, these researches has been discontinued. Combination of RO4929097 and bevacizumab was well tolerated in phase I of clinical trial and can be considered in patients with recurrent malignant glioma.

LANIQUIDAR is a P-glycoprotein inhibitor. It was used in trials studying the treatment of breast cancer.

Mipitroban (previously known as UP 11677), a thromboxane A2 receptor antagonist that was investigated to treat thrombosis. However, further studies were apparently discontinued.

Daniquidone, also known as Batracylin, is a water-insoluble heterocyclic amide with potential antineoplastic activity. Daniquidone inhibits topoisomerases I and II, thereby inhibiting DNA replication and repair, and RNA and protein synthesis. Batracylin advanced as an anticancer agent to Phase I clinical trials where dose limiting hemorrhagic cystitis (bladder inflammation and bleeding) was observed.

Pentiapine is a dopamine release inhibitor. It is a tranquiliser. Pentiapine produces a dose-dependent decrease in spontaneous motor activity and blocks the morphineinduced hyperactivity. Moreover, this drug in itself has no effect on place conditioning but blocks the acquisition of morphine-induced conditioned place preference.