Cinobufotalin, the bufadienolide isolated from toad venom, has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane potential decrease, and reactive oxygen species (ROS) production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice daily, for 7 days) significantly inhibited A549 xenograft growth in mice. Further, same cinobufotalin administration improved mice survival at week five. Cinobufotalin administration didn’t significantly affect mice body weight, indicating the relative safety of this regimen. Thus, cinobufotalin inhibits A549 xenograft growth in vivo and improves mice survival.

Edogesterone (PH-218) is steroid with progestational and antiandrogenic properties.

Fucoxanthin isis a marine carotenoid mainly found in brown algae, giving them a brown or olive-green color. Fucoxanthin is investigated for its anti-inflammatory, antinociceptive and anti-cancer effects. In vivo studies have demonstrated that oral administration of fucoxanthin inhibited carcinogenesis in an animal model of duodenal, skin, colon and liver cancer. Fucoxanthin causes antitumor and anticarcinogenic effects by inducing G1 cell-cycle arrest and apoptosis by modulating expression of various cellular molecules and cellular signal transduction pathways, but the exact mechanism of anti-cancer action of fucoxanthin is not fully elucidated. Fucoxanthin regulates lipids metabolism, the effect most likely mediated by AMK-activated protein kinase. A clinical trial of fucoxanthin against non-alcoholic fatty liver disease is ongoing.

Esoxybutynin is (S)-enantiomer of oxybutynin. Esoxybutynin exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.