Edotecarin (J-107088 or [6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carb azo le-5,7(6H)-dione]) is a DNA topoisomerase I inhibitor. The antitumor activity of edotecarin has been tested in vitro and in vivo, and inhibition of tumor growth has been observed in breast, cervix, pharynx, lung, prostate, colon, gastric, and hepatic cancer models. Banyu Pharmaceutical Co Ltd and Pfizer Inc were developing edotecarin for the potential treatment of solid tumors. Edotecarin development has been discontinued.

An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. Gandotinib is in phase II clinical trials by Lilly for the treatment of myeloproliferative disorders.

Darapladib (SB-435495), as reversible inhibitors of lipoprotein-associated phospholipase A(2) (Lp-PLA(2) has been developed and studies for the potential treatment of atherosclerosis. In November 2013, GSK announced that the drug had failed to meet Phase III endpoints in a trial of 16,000 patients with acute coronary syndrome.

Edotreotide (SMT487) is a DOTA-containing somatostatin analog. Edotreotide binds with high affinity to somatostatin receptors. Somatostatin receptors are predominantly overexpressed by neuroendocrine tumors. On 15 September 2016, the European Medicines Agency’s Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion, recommending granting a marketing authorisation for the orphan medicine edotreotide (SomaKit-TOC) intended for use in Positron Emission Tomography (PET) imaging in adult patients with gastro-enteropancreatic neuroendocrine tumours (GEP-NETs). SomaKit TOC was designated as an orphan medicinal product on 19 March 2015. 68Ga-Edotreotide, distributed under the brand name TOCscan® (Sogacin® in Austria/ France), is the companion diagnostic in ITM´s theranostic approach for the treatment of neuroendocrine tumors (NETs). N.c.a. 177Lu-Edotreotide is known as an innovative Targeted Radionuclide Therapy agent with favorable safety profile and promising efficacy. N.c.a. 177Lu-Edotreotide received an Orphan Designation as treatment of gastro-entero-pancreatic neuroendocrine tumors (GEP-NET) based on academic clinical Phase II data suggesting a significant benefit (substantially improved progression-free survival, PFS).