Wilex developed WX-UK1 as a specific inhibitor of human trypsin-2, human trypsin-3 and urokinase-plasminogen activator. WX-UK1 participated in phase I clinical trial in combination with capecitabine in advanced malignancies to determine the safety, tolerability, maximum tolerated dose, pharmacokinetics, and pharmacodynamics. However, in April 2014, the clinical development of this drug was discontinued, as part of a company restructure.

Fasitibant (MEN-16132) is a non-peptide sulfonamide-containing bradykinin hB2 receptor antagonist. It inhibits pro-inflammatory response in vitro and alleviates inflammatory hyperalgesia in rodent models of osteoarthritis. Menarini Group was developing fasitibant for the treatment of osteoarthritis. Fasitibant development has been discontinued.

Atecegetran metoxil (more widely known as AZD0837), an anticoagulant and a prodrug, converted to a selective and reversible direct thrombin inhibitor (AR-H067637). Atecegetran metoxil participated in phase II clinical trials to prevent the stroke and systemic embolism in patients with non-valvular atrial fibrillation. The development of atecegetran metoxil was discontinued, due to a limitation identified in the long-term stability of the extended-release drug product.

PQR-309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR-309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. By inhibiting mTOR to a lesser extent than PI3K, PQR-309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy. PQR-309 is in phase II clinical trial for the treatment of glioblastoma, head and neck cancer, lymphoma and breast cancer. Common adverse events included fatigue, hyperglycemia, nausea, diarrhea, constipation, rash, anorexia and vomiting.

Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.

BNC105P, a vascular disrupting agent, is a disodium phosphate ester prodrug of BNC105. BNC105P is a tubulin polymerization inhibitor that suppresses cancer cell proliferation. BNC105P participated in phase I/II trial for patients with metastatic renal cell carcinoma. Although the primary endpoint was not met in an unselected population, correlative studies suggested several biomarkers that warrant further prospective evaluation. Besides, BNC105P was involved in phase II clinical trial as second-line chemotherapy for advanced malignant pleural mesothelioma. The drug was safe and tolerable, but the sole response was insufficient to warrant further research as a single agent. In addition, BNC105P in combination with Ibrutinib was studied in phase I trials for patients with chronic lymphocytic leukemia to determine the preliminary assessment of the efficacy.

Briciclib (also known as ON-013105 and ON-014185) has the potential of targeting and inhibition of eukaryotic translation initiation factor 4E (eIF4E) for solid cancers. eIF4E is a proto-oncogene that promotes translation of several genes essential for cellular proliferation (cyclin D1, c-Myc, mTOR), survival (Akt), angiogenesis (VEGF), and metastasis (MMP9). Overexpression of eIF4E has been observed in almost all major groups of cancers and has been shown to induce increased expression of cyclin D1 and c-Myc). An intravenous formulation of briciclib was being investigated in the Phase 1 clinical trial. The purpose of the study was to determine the highest dose of briciclib that could be given safely in patients with relapsed/refractory Lymphoma or B-cell Acute Lymphocytic Leukemia (Philadelphia chromosome negative). However, this study was terminated because of the lack of available clinical drug supply. In addition, briciclib was also involved in phase I clinical trials with advanced cancer and solid tumors, to determine the highest dose that can be safely given.

Bradanicline (formerly known as ATA-101 or TC-5619), a selective full agonist for the alpha7 neuronal nicotinic receptor (NNR) subtype was developed for the treatment of central nervous system diseases and disorders. Bradanicline participated in phase II clinical trials for patients with negative and cognitive symptoms of schizophrenia; however, results did not support a benefit of the drug. The development was also discontinued for Alzheimer's disease and attention-deficit hyperactivity disorder. In addition, it was announced that the first patient had been treated in Phase 2 clinical trial in chronic cough with bradanicline. Phase 2 will test the efficacy and safety of bradanicline in up to 49 patients with refractory chronic cough. Refractory chronic cough is defined as a cough that persists for eight weeks or more. In the plans will conduct additional clinical trials to test the safety and efficacy of bradanicline.

MK-2206 is an oral selective allosteric inhibitor of Akt that targets all three isoforms of human Akt (Akt-1, Akt-2 and Akt-3). In a phase I study of solid tumors, MK-2206 demonstrated evidence of target modulation and anti-proliferative activity as a single agent and in combination with other agents. Current ongoing trials of MK-2206 include monotherapy and combination therapy in breast cancer, colorectal cancer, haematological malignancies, non-small cell lung cancer and other. Detected treatment-related adverse event are: rash, fatigue, hyperglycemia.