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.

Carnosol is an ortho-diphenolic diterpene with an abietane carbon skeleton with hydroxyl groups at positions C-11 and C-12 and a lactone moiety across the B ring. Carnosol is the product of oxidative degradation of carnosic acid. Carnosol is a naturally occurring phytopolyphenol found in rosemary that functions as an antioxidant, antimicrobial, and anticarcinogen. Carnosol has been shown to inhibit inductions of COX-2 by blocking PKC signaling. Carnosol is an inhibitor of AR and ER α. Several pre-clinical studies have suggested that carnosol selectively targets tumorigenic cell as opposed to non-tumorigenic cells and is safe and tolerable in animals. Carnosol has been shown to elicit chemopreventive effects by (1) blocking the bioactivation of carcinogens, (2) enhancing antioxidant and/or detoxification enzyme activities, (3) suppressing tumor-promoting inflammation, (4) inhibiting cell proliferation and inducing apoptosis selectively in cancer cells, and (5) blocking tumor angiogenesis and invasion.

The immunosugar N-9-methoxynonyldeoxynojirimycin (SP-187, UV-4B) is an inhibitor of both glucosidases I and II. In preclinical studies, it displayed inhibition of dengue and influenza virus infection. The compound developed by Emergent BioSolutions and evaluated in phase 1 clinical trials on healthy subjects.

Trantelinium bromide is an anticholinergic and spasmolytic drug, used for the treatment of gastric ulcers.