Palytoxin is the most potent marine toxin known that was isolated from a zoanthid of the genus Palythoa and Cyanobacteria (Trichodesmium). Palytoxin is a potent vasoconstrictor that damages the ionic gradient of the cells, causing cell death. This toxin has a strong potential for toxicity in humans and animals that is why it causes great concern worldwide. It is crucial to remove this toxin and start an aggressive topical therapy as soon as possible.

Cofisatin is a synthetic derivative of a dehydrocholic acid and isatine, invented by French Societe D'etudes et Applications Chimiques in the 1950s. The compound is claimed to promote intestinal peristaltic without causing irritation.

Vinformide (also known as N-formylleurosine), an N-formyl analog of leurosine possesses antineoplastic activity. This drug was studied for the treatment of lymphoma, leukemia and Hodkin’s disease. However, studies were discontinued, because vinformide exerted an acute cardiotoxic side effect.

Solamargine is the one of major compounds of Solanum lycocarpum- fruit glycoalkaloid extract, and a major steroidal alkaloid glycoside, which is purified from Solanum nigrum L (SNL), a traditional Chinese medicinal herb. It has been shown that solamargine has anti-tumor activity against the several types of cancers. Also as a part of SR-T100 Gel solamargine in the phase II of clinical trial for the treatment of Actinic Keratosis and Bowen's Disease. The precise mechanism of its actions is still undefined, but existed several potential pathways. In case of castration-resistant prostate cancer cells, solamargine inhibits the growth cells through AMPKalpha-mediated inhibition of p65, followed by reduction of MUC1 expression in vitro and in vivo. In case of lung cancer cells solamargine inhibits the growth cells through reduction of EP4 protein expression, followed by increasing ERK1/2 phosphorylation. The inter-correlations between EP4, DNA methyltransferase 1 (DNMT1) and c-Jun and feedback regulation of ERK1/2 by c-Jun contribute to the overall responses of solamargine in this process.

EP-217609 is a new synthetic parenteral dual-action anticoagulant combining a direct thrombin inhibitor (α-NAPAP analog), an indirect factor Xa inhibitor (fondaparinux analog) and a biotin moiety allowing its neutralisation. EP-217609 is the biotinylated form of EP42675. As announced in May 2009, EP42675 has successfully completed a phase I program in 100 healthy subjects. EP42675 was well tolerated and showed predictable pharmacokinetic (PK) and pharmacodynamic (PD) profiles with low intra- and intersubject variabilities. In animals, the PK/PD profiles of EP-217609 and EP42675 are similar. EP-217609 exhibited similar in vitro anticoagulant properties as its parent compounds. EP-217609 exhibits an unprecedented pharmacologic profile in showing high bioavailability, long plasma half-life, and potent antithrombotic activity in animals without the complications of thrombin rebound. EP-217609 is administered intravenously or subcutaneously at fixed dose without need for monitoring. EP-217609 was in Phase-II clinical trials in thrombosis prevention in France (IV), but development of EP-217609 appears to have been discontinued.

NSC-631570 (Ukrain) is a semisynthetic compound of thiophosphoric acid and the alkaloid chelidonine from the plant Chelidonium majus. Ukrain was promoted as a drug to treat cancer and viral infections, including HIV and hepatitis. It exerts a selective cytotoxic effect on tumor cells in vitro and in vivo and shows the ability to modulate immunocyte functions. Ukrain has been used in complementary herbal medicine for more than 20 years for the treatment of benign and malignant tumors. Thus, in unresectable advanced pancreatic cancer, Ukrain alone and in combination with gemcitabine nearly doubled the median survival times in patients suffering from advanced pancreatic cancer. Inhibition of the growth of cancer cell lines in vitro, tumor mass reductions in vivo, and partial and complete remissions in oncological patients, occur as a result of Ukrain application. The drug may interfere directly with the metabolism of cancer cells and it also improves the functioning of the host immune system. Diminished synthesis of DNA, RNA and proteins, the inhibition of cellular oxygen consumption, and the induction of programmed cell death in malignant cells have been described following Ukrain administration. The drug can also modify the immunological response via an increase in the number of total T-cells and a normalization of the T-helper/T-suppressor lymphocyte ratio. However,according to the American Cancer Society and the Memorial Sloan-Kettering Cancer Center, there is no evidence that Ukrain is an effective cancer treatment. Through an Austrian company known as Nowicky Pharma, the drug, which was never approved by regulators, was sold as a treatment for AIDS, radiation-induced diseases and as a cure for all forms of cancer. Ukrain is not approved by the Food and Drug Administration but is available in parts of Europe and from Tijuana clinics.

Avicin D, a natural triterpenoid saponin, is a selective glucocorticoid receptor (GR) modulator. It has been approved by the United States Food and Drug Administration for phase I studies in human cancer patients. In addition, avicin D has the therapeutic potential for patients with Sézary syndrome.