AZD0424, a dual selective Src/Abl kinase inhibitor that has shown evidence of anti-tumor activity in pre-clinical studies. AZD0424 participated in phase I clinical trials in patients with advanced solid tumors, but this study was terminated because of insufficient evidence of efficacy as monotherapy.

Ajulemic acid, designated as Resunab™, is being developed by Corbus Pharmaceuticals, for the treatment of cystic fibrosis, systemic sclerosis, systemic lupus erythematosus.Ajulemic acid (AJA) is a first-in-class, synthetic, orally active, cannabinoid-derived drug that preferentially binds to the CB2 receptor and is nonpsychoactive. In preclinical studies, and in Phase 1 and 2 clinical trials, AJA showed a favorable safety, tolerability, and pharmacokinetic profile. It also demonstrated significant efficacy in preclinical models of inflammation and fibrosis. It suppresses tissue scarring and stimulates endogenous eicosanoids that resolve chronic inflammation and fibrosis without causing immunosuppression. AJA is currently being developed for use in 4 separate but related indications including systemic sclerosis (SSc), cystic fibrosis, dermatomyositis (DM), and systemic lupus erythematosus. Phase 2 clinical trials in the first 3 targets demonstrated that it is safe, is a potential treatment for these orphan diseases and appears to be a potent inflammation-resolving drug with a unique mechanism of action, distinct from the nonsteroidal anti-inflammatory drug (NSAID), and will be useful for treating a wide range of chronic inflammatory diseases.

CC-223 is an orally available inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. CC-223 disrupted mitochondrial function, and induced mitochondrial permeability transition pore (mPTP) opening and reactive oxygen species (ROS) production. CC-223 is currently in phase II clinical trials for the treatment of Multiple myeloma; Non-Hodgkin's lymphoma; Solid tumours. The most common treatment-related adverse events were hyperglycemia, fatigue and rash.

Depramine is a dibenzazepine derivative. Its chemical structure is related to imipramine and it has antidepressant effects as well as anti-Parkinson effects. Dimepramine fumarate is an anticholinergic agent and inhibits the uptake of norepinephrine. The anticataleptic effect of dimepramine fumarate is attributed to its anticholinergic properties and to its probable role in central adrenergic and/or dopaminergic stimulation. The drug tends to decrease autonomic arousal responses of Parkinson patients as measured by resting conductance levels, number of fluctuations in skin conduction per minute, orienting response, and habituation rate. Depramine is used for the treatment of obsessive compulsive disorder, obsessions and phobias, panic disorder, cataplexy associated with narcolepsy, major depressive disorder, and chronic pain. It can help ease the symptoms in each of these conditions. It works by interfering with the brain chemical serotonin. Side effects of depramine are: dizziness, irritability, blurred vision, dry mouth, nausea or vomiting, swelling of face and feet, acid or sour stomach, constipation, shaking of hands or feet, mouth ulcers, irregular menstrual periods.

QAV-680 is a pyrrolopyridine derivative patented by Novartis Pharma GmbH as chemoattractant receptor (CRTh2) antagonist for the treatment of an inflammatory or allergic condition, particularly an inflammatory or obstructive airways disease. QAV-680 shows low nM potency and excellent selectivity across a range of CRTh2 dependent primary human inflammatory cell assays. In preclinical studies, QAV-680 shows good pharmacokinetic properties (including a suitable escalating dose–exposure relationship) in the rat and mouse and demonstrates efficacy in both mechanistic and allergic disease CRTh2-dependent rodent in vivo models. In 2008-2010 QAV-680 was tested in Phase 2 clinical trials but no further development reports were published.