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.

Delmitide is the decapeptide with antiinflammatory activity. It is the first low molecular weight compound inhibiting TNF production at a translational level. Also, delmitide inhibits production of IFN-gamma, IL-12 and IL-2. It targets TRAF6/IRAK4/MyD88 complex and inhibits phosphorylation of SAPKs (p38 and JNK). Delmitide inhibits AP1 and NFkB activation. Delmitide was developed for the potential treatment of Crohn's disease and ulcerative colitis; phase II trials for both these indications commenced in October 2001. Phase I trial in chemotherapy-induced diarrhea and the gastrointestinal complications of HIV were also initiated. However, no recent development has been reported.

Depreotide is an ingredient in the diagnostic aid (radioactive imaging agent). Technetium Tc 99m labeled depreotide is a scintigraphic imaging agent that identifies somatostatin receptor-bearing pulmonary masses in patients presenting with pulmonary lesions on computed tomography and/or chest x-ray who have known malignancy or who are highly suspect for malignancy. Adverse events were evaluated in clinical studies of 647 adults. Deaths did not occur during the clinical study period. After Technetium Tc 99m Depreotide Injection, serious adverse events were not reported. Headache was the most commonly reported adverse event. EMA withdrew depreotide containing agent NeoSpect.

Edratide (hCDR1 or TV-4710) is a peptide based on the sequences of the complementarity determining region (CDR) 1 of monoclonal anti-DNA antibody. The capacity of the peptide to bind to major histocompatibility complex class II molecules correlated with the proliferative responses. Edratide is being developed for the treatment of SLE (Systemic Lupus Erythematosus). Edratide ameliorates the SLE-related autoimmune process by specific upstream immunomodulation through the generation of regulatory T cells.

PNU-96391A (known as OSU6162) is a weak dopamine (DA) D(2) receptor antagonist with behavioral stabilizing properties. OSU6162 seem to act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling (partial agonist on 5-HT2A receptor). OSU6162 in a phase II European clinical trial in treatment of Myalgic Encephalomyelitis/Chronic Fatigue Syndrome. One of the isomer of OSU 6162, has promise for treating Parkinson's disease, Huntington's disease and schizophrenia, but both enantiomers of OSU 6162 had dual effects on behavior, stimulating locomotor activity in 'low activity' animals and inhibiting locomotor activity in 'high activity' animals.