Octamoxine (ximaol), a monoamine oxidase inhibitor was used as an antidepressant to treat mental depression. Now this drug is no longer marketed.

A small molecule, multi-target kinase inhibitor, 4SC-203 (formerly SC-71710), was being developed by 4SC AG for the treatment of cancer, with an focus on acute myeloid leukaemia. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs). This may result in the inhibition of angiogenesis and cell proliferation in tumor cells in which these kinases are upregulated. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias (AML). VEGFRs, tyrosine kinase receptors, are overexpressed in a variety of tumor cell types and play key roles in angiogenesis. 4SC has discontinued the development of 4SC-203 (formerly SC-71710), the lead in a series of Flt-3, VEGF protein kinase and aurora kinase A and B inhibitors, for the treatment of acute myeloid leukaemia (AML) as the personnel and financial resources have been allocated preferentially to the development of resminostat.

The carotenoids lutein (L), zeaxanthin (Z), and meso-zeaxanthin (MZ) accumulate in the central retina, where they are collectively known as macular pigment (MP). Each of these three compounds exhibit a regional dominance, with MZ, Z, and L being the dominant carotenoids at the epicenter, mid-periphery, and periphery of the macula, respectively. Meso-zeaxanthin is formed directly in the retina from lutein. MZ has potent anti-inflammatory effect, which can be due to its down-regulated expression of various inflammatory mediator genes. Meso-zeaxanthin was also found to scavenge superoxide radicals, hydroxyl radicals. MZ is a part of formulation for MacuShield, which is now the UK’s most recommended eye supplement. Also exists experiments supporting that LMZ3 (meso-zeaxanthin, lutein, zeaxanthin) supplements may stabilize vision and improve the cavitation’s in patients with macular telangiectasia type 2.

AZD-3759 is an oral inhibitor of both wild-type and mutant EGFR with IC50 values in nanomolar range. The drug was discovered by AstraZeneca for the treatment of non-small-cell lung cancer with CNS metastases. AZD-3759 can penetrate the blood-brain barrier and was confirmed to be effective in vitro with NSCLC cell lines as well as in mouse model of brain metastases. AZD-3759 is currently in Phase 1 clinical trial.

ETC-159 (ETC-1922159) is an inhibitor of membrane-bound O-acyltransferase porcupine. Porcupine palmitoleates Wnt and this modification is essential for binding to chaperone WLS and Frizzled receptors and is therefore required for the activity of all Wnts. ETC-159 exerts antineoplastic properties both in vitro and in vivo due to inhibition of Wnt pathway. ETC-159 development has progressed to phase I clinical trial.