ITURELIX, a decapeptide, is a gonadotropin-releasing hormone antagonist.

Dotefonium is the anticholinergic, spasmolytic agent.

Serfibrate, a clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is a hypolipidemic agent.

Tafluposide (also known as F 11782) is an epipodophyllotoxin derivative patented by Pierre Fabre Medicament as an antitumor agent. Tafluposide acts as a catalytic inhibitor of topoisomerases I and II, that capable of completely inhibiting the DNA-binding activity of topoisomerase. In preclinical models single or multiple i.p. doses of Tafluposide proves highly active against the s.c. grafted B16 melanoma, significantly increasing survival and inhibiting tumor growth. Tafluposide inhibits the number of pulmonary metastatic foci of the melanoma by 99%. In human tumor xenograft studies, multiple i.p. doses of Tafluposide results in major inhibitory activity against breast) tumors, as well as causing definite tumor regression. Significant activity was also recorded Tafluposide against the refractory lung xenografts.

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).

Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.

Cinepaxadil is cinnamoyl-piperazine derivative developed by Delalande SA for treatment cardiovascular system disorders. Cinepaxadil decrease dogs cardiac activity after i.v. administration.