GW-493838 was developed by GlaxoSmithKline as an adenosine A1A receptor agonist for the treatment of dyslipidemia and neuropathic pain. GW493838 participated in the phase II clinical trial to determine the analgesic effect in patients with post-herpetic neuralgia or peripheral nerve injury caused by trauma or surgery. However, this study has been discontinued.

Cipargamin is an experimental synthetic antimalarial molecule belonging to the spiroindolone class. It possesses both the potency (average IC50 of 550 pM against asexual blood-stage P. falciparum) and favorable pharmacokinetics (elimination half-life of ~24 hours in humans) needed for a single-dose cure, a feature that could help slow the onset of parasite resistance and that is not shared by existing, approved antimalarial drugs. KAE609 is also unique in its ability to block transmission to mosquitoes. Cipargamin is a parasite P-type ATPase4 inhibitor. Cipargamin in phase II clinical trials for the treatment of acute, uncomplicated malaria due to plasmodium falciparum monoinfection. Nausea was the most common reported adverse effect. The adverse events were generally mild and did not lead to any discontinuations of the drug.

Lexanopadol is a potent ORL-1 agonist (opioid receptor like -1), nociceptin receptor agonists and opioid mu receptor agonists. Preliminary evidence suggests that targeting ORL-1 receptors may have synergistic effects with mu receptors hence enhancing the therapeutic profile of Lexanopadol in the treatment of pain. Lexanopadol is particularly suited for the management of moderate to severe chronic pain, including neuropathic pain. Lexanopadol hemicitrate is in phase II clinical trials for the treatment of pain. However there is no recent development reported.

AMG-925, a dual FLT3/CDK4 inhibitor, has been developed to overcome resistance to FLT3 inhibitors, which is a serious clinical issue in treating acute myelogenous leukemia (AML). AMG-925 inhibits FLT3, including many FLT3 mutants reported to date. AMG-925 inhibits the proliferation of a panel of human tumor cell lines including Colo205 (Rb(+)) and U937 (FLT3(WT)) and induced cell death in MOLM13 (FLT3(ITD)) and even in MOLM13 (FLT3(ITD, D835Y)), which exhibits resistance to a number of FLT3 inhibitors currently under clinical development. At well-tolerated doses, AMG-925 leads to significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation. AMG-925 is in Phase I clinical trials for the treatment of Acute myeloid leukaemia.

Sevitropium is a bronchospasmolytic agent.

Lunasine is an alkaloid present in bark and leaves of Lunasia quercifolia (Rutaceae). It does not relate to bioactive peptide lunasin isolated from soybean.

Neoandrographolide, one of the principal diterpene lactones, isolated from a medicinal herb Andrographis paniculata Nees. Andrographis paniculata (Burm. f.) Wall. ex Nees (Acanthaceae), also known as “kalmegh” in India, is a widely distributed plant in Asia. In many traditional formulations, the aerial parts have been used as anti-inflammatory and antipyretic drugs for the treatment of a variety of chronic and infectious diseases. Neoandrographolide possesses significant anti-inflammatory effects, which implies that it would be one of the major contributing components to participate in the anti-inflammatory effect of A. paniculata. and a potential candidate for further clinical trial.