(+)-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.

Deximafen is antidepressant drug developed by Abbot Laboratories Inc.

Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.

Timelotem is a benzodiazepine derivative patented by Kali-Chemie Pharma G.m.b.H. as an anesthetic agent. In preclinical models, Timelotem shows atypical antipsychotic activity. Timelotem antagonizes DL-2-amino-5-phosphonovaleric acid (AP-5)-induced sniffing and the body turns in rats. Further, Timelotem antagonized amphetamine-induced stereotyped behavior in rats but was found less active than haloperidol in this test.

Timelotem is a benzodiazepine derivative patented by Kali-Chemie Pharma G.m.b.H. as an anesthetic agent. In preclinical models, Timelotem shows atypical antipsychotic activity. Timelotem antagonizes DL-2-amino-5-phosphonovaleric acid (AP-5)-induced sniffing and the body turns in rats. Further, Timelotem antagonized amphetamine-induced stereotyped behavior in rats but was found less active than haloperidol in this test.

Tomivosertib (eFT-508) is a dual inhibitor of MAP kinase-interacting kinases (MNK1 and MNK2) thereby controlling translation. It has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors. Tomivosertib acts on multiple points in the cancer immunity cycle simultaneously, underscoring its therapeutic potential as both a monotherapy and in combination with existing checkpoint inhibitor treatments. Preclinical studies suggest combining tomivosertib with a checkpoint inhibitor can overcome mechanisms of resistance to checkpoint inhibitors, resulting in enhanced sensitivity to checkpoint inhibitors and a higher response rate. In addition, preclinical data demonstrate that tomivosertib as a single agent promotes antitumor immunity that persists after stopping drug treatment. Tomivosertib is currently being evaluated in Phase 2 clinical trials in solid tumors and lymphoma. Additionally, tomivosertib may be a new therapeutic for neuropathic pain.

BL-1021 was developed by BioLineRx Ltd. for the treatment of neuropathic pain or pain that results from damage to nerve fibers. The drug has completed phase I clinical trials, however further information is not available.