APC-3316 is a vinyl sulfone cystein protease inhibitor. It is a potent, irreversible cysteine protease inhibitor and a potent and selective CCR4 antagonist. Its therapeutic targets are cruzain, a cysteine protease of the protozoan parasite Trypanosoma cruzi, and cathepsins B and L, which are associated with cancer progression. It was discontinued after preclinical trials in Chagas disease in USA.

MCD-386CR (CDD-0102A) is a functionally selective agonist with partial agonist activity at M1 muscarinic receptors, weak activity at M3 receptors, and no activity at other muscarinic receptor subtypes. In preclinical studies, it enhances memory function in animal models of Alzheimer's disease. MCD-386CR (CDD-0102A) received orphan drug designation from FDA in 2011. The drug is intended to treat progressive supranuclear palsy, a degenerative brain disease that affects balance, walking, speech, cognition, and eye movements.

Diethylnorspermine is the structural analog of polyamines. Polyamines were shown to downregulate polyamine synthesis and uptake, upregulate polyamine catabolism, and result in a profound depletion of polyamines. Diethylnorspermine is adenosylmethionine decarboxylase, ornithine decarboxylase inhibitor and spermidine-spermine N1-acetyltransferase stimulant. Diethylnorspermine is under investigation as a novel anticancer drug for a variety of neoplasms. It has sustained inhibitory effects on the growth of human prostate carcinoma cells in vitro as well in vivo. This polyamine analog may provide a new tool in the chemotherapy of prostate cancers with various phenotypes. Diethylnorspermine was relatively well tolerated in patients with advanced hepatocellular carcinoma (HCC) including those with mild-to-moderate liver dysfunction but further evaluation of diethylnorspermine monotherapy for advanced HCC does not appear to be justified because of insufficient evidence of clinical benefit in the patients evaluated in this study. Also, no evidence of clinical activity was detected in metastatic breast cancer treatment (phase II clinical study).

TAK-603 is a quinoline derivative, originally developed as a anti-rheumatic drug. TAK-603 selectively suppresses Th1 cytokine production. In animal models TAK-603 has the ability to suppress the immune system and protect cartilage from destruction. The development of TAK-603 has been discontinued.