Defoslimod is an analog of lipopolysaccharide endotoxin-derived lipid A obtained from E. coli, developed as an immunomodulatory adjuvant and an immunotherapeutic agent for the treatment of cancer. Defoslimod acts as an agonist of Toll-like receptor (TLR) 2/4. In a phase 1 clinical study in patients with solid tumors, conducted in 2007, defoslimod was administered as an intravenous infusion. The therapy was well tolerated at biologically active concentrations, with 3 patients of 17 exhibited disease stabilization with a mean duration of 4 months. No further development of the drug was reported.

Scopoletin is a coumarin that can be isolated from plants of the genus Scopolia. It has been identified as a natural antifungal compound. Scopoletin was also demonstrated to be an MAO inhibitor capable of increasing dopamine levels in mice and is therefore of potential interest for developing treatments for neurodegenerative diseases.

Swainsonine is an indolizidine alkaloid found in Australian Swainsona canescens, North American plants of the genera Astragalus and Oxytropis and also in the fungus Rhizoctonia leguminocola. It is competitive inhibitor of Golgi alpha-mannosidase II and lysosomal alpha-mannosidases. This compound has been reported to be a potent antiproliferative and immunomodulatory agent. However, no evidence of anti-tumor activity of swainsonine was seen in phase II clinical trial, in patients with locally advanced or metastatic renal cell carcinoma. Adverse events such as fatigue, nausea and diarrhea were common but generally mild. Swainsonine is locoweed toxin. Locoweed poisoning is seen throughout the world and annually costs the livestock industry millions of dollars. Swainsonine inhibits lysosomal alpha-mannosidase and Golgi mannosidase II. Poisoned animals are lethargic, anorexic, emaciated, and have neurologic signs that range from subtle apprehension to seizures.

Nisterime is a dihydrotestosterone derivative. Nisterime acetate (ORF-9326) was shown to inhibit implantation in several species. It is also interrupts the postimplantation stage of gestation.

KP-1461 is a prodrug of KP-1212, an antiviral agent developed for the treatment of human immunodeficiency virus (HIV) infection. KP-1212 induces an increase in the HIV mutation rate thus leading to viral ablation.

Orpanoxin (previously known as F-776), a nonsteroidal anti-inflammatory drug that was developed as an analgesic agent. Orpanoxin is a prostaglandin synthetase inhibitor and may have a potential for the treatment of rheumatic. However, information about the current development of this drug is not available.