Oxeclosporin (previously known as SDZ IMM 125 and now called as tigderimus) was developed as an immunosuppressive drug. It was shown that the drug possessed apoptotic activity via induction of uptake of extracellular calcium. The increased intracellular calcium might directly cause apoptosis by increasing the caspase-3 activity. Oxeclosporin was studied in clinical trials in patients with severe psoriasis. In addition, it was used for the treatment of rheumatoid arthritis and transplant rejection. However, all these studies were discontinued. Besides, oxeclosporin is participating in phase II trials in Europe for the treatment of asthma and in Switzerland for the treatment of cancer. However, information about the further development of this drug is not available.

Detirelix is a synthetic decapeptide containing five D-amino acids. It is a very potent Gonadotropin-releasing hormone (GnHR) antagonist. The acute effects of detirelix were consistent with peripheral vasodilation. Subchronic effects were associated with inhibition of pituitary gonadotropic and gonadal hormone secretion. As long-acting GnRH antagonist detirelix can rapidly suppress gonadotropin secretion, inhibit follicular development, and prevent ovulation. It can be used as luteolytic agent. A projected use is for the treatment of sex hormone-releasing diseases, as part of anticancer hormone therapy of sex-hormone-dependent tumors.

ABT-510 is an anti-angiogenesis compound that was under development by Abbott for the treatment of solid tumours, lymphoma and melanoma. It is a synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).

N-acetylmannosamine (ManNAc), a hexosamine monosaccharide, is the first committed biological precursor of Neu5Ac. N-acetylmannosamine is being investigated as a potential treatment for GNE myopathy. N-acetylmannosamine has being reported to improve the cognitive function in aged animals. It has potential therapeutic application for cognitive dysfunction. N-acetylmannosamine is under investigation for GNE myopathy.

LTX-315 is a cationic amphipathic peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis. The oncolytic effect of LTX-315 involves a unique immunogenic cell death targeting the mitochondria with subsequent release of danger-associated molecular pattern molecules. This initial targeting of the mitochondria is followed by disintegration of other cytoplasmic organelles resulting ineffective release of additional danger signals and a broad repertoire of tumour antigens and finally lysis of plasma membrane (necrosis). Preclinical and clinical studies have demonstrated LTX-315`s unique ability to reshape the tumour microenvironment by inducing the effective release of danger signals, chemokines and a broad repertoire of tumour antigens. These properties of LTX-315 results in enhanced infiltration of activated CD 8 T cells and Th1 responses. This ability to convert non-T cell inflamed tumours to T cell inflamed tumours makes LTX-315 an ideal combination partner with other types of immunotherapy, including immune checkpoint inhibitors/agonists, vaccines, and T cell-based therapies. Both preclinical and clinical studies have confirmed LTX-315s ability to induce a systemic anticancer immune response when injected locally into tumours resulting in complete or partial regression of injected and non-injected tumours (i.e. abscopal effect). Preclinical studies have demonstrated strong synergy with immune-checkpoint blockade which have given the scientific rationale for initiating combinations studies with Ipilimumab and Pembrolizumab in melanoma and TNB cancer patients respectively. Phase Ib study combining LTX-315 with ipilimumab (anti-CTLA4) in malignant melanoma patients, as well as LTX-315 with pembrolizumab (anti-PD-1) in metastatic breast cancer patients, is ongoing.

Ceralasertib, previously known as AZD6738, a potent and selective inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase was developed as an anticancer agent. Prevention of ATR-mediated signaling leads to the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. AZD6738 as a combination therapy participates in phase II clinical trials for the treatment of gastric adenocarcinoma and malignant melanoma (in combination with durvalumab). For the treatment of gastric and breast cancer in combination with carboplatin, or with olaparib or with MEDI4736. Combination of acalabrutinib and AZ6738 is used in phase II trials for patients with chronic lymphocytic Leukemia. Besides, AZD6738 participates in umbrella Phase II study in patients with metastatic non-small cell lung cancer (NSCLC) who have progressed on an anti-programmed cell death-1/anti-programmed cell death ligand 1 (anti-PD-1/PD-L1) containing therapy.