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.

A-TRISACCHARIDE (or Blood group A trisaccharide), a core antigen fragment in ABO blood group system. It was found to be a major urinary carbohydrate depending on diet and blood type.

INO-4995, a synthetic analog of the intracellular signaling molecule, D-myo-inositol 3,4,5,6-tetrakisphosphate, regulates airway secretory and absorptive processes, affecting mucosal hydration by prolonged inhibition of Na(+) and fluid absorption in cystic fibrosis (CF) human nasal epithelia. At the moment INO-4995 is in preclinical development for CF treatment.

GGTI-2418, also known as PTX100, is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways. In preclinical studies, GGTI-2418 has been shown to cause significant breast tumor regression in ErbB2 transgenic mice model. GGTI-2418 was the first GGTase I inhibitor to enter clinical development in early 2009. Phase I clinical trials early results demonstrated that ~30% of patients with advanced solid tumors had stable disease following GGTI-2418 therapy, the compound was well-tolerated and had minimal toxicity. However, the Phase I trial of GGTI-2418 has been stopped due to its lack of efficacy in patients. In February 2015 Prescient Therapeutics in-licensed the p27 biomarker for use as a companion diagnostic. Patients with low levels of p27 are more likely to respond to GGTI-2418 therapy.

7β-hydroxycholesteryl-3-oleate has been shown to inhibit astrogliosis and intracranial glioblastoma growth. Local administration of 7β-hydroxycholesteryl-3-oleate inhibits growth of experimental rat C6 glioblastoma. These data suggest that 7β-hydroxycholesteryl-3-oleate might be useful for local glioblastoma chemotherapy. 7β-hydroxycholesteryl-3-oleate is a potent inhibitor of the endogenous cholesterol biosynthesis in brain showing a correlation between cholesterogenesis and reactive astrocyte proliferation. 7β-hydroxycholesteryl-3-oleate can reduce the astrocytic reaction following spinal cord injury, promoting the serotonergic reinnervation of a denervated territory. On 17 December 2010, orphan designation (EU/3/10/816) was granted by the European Commission to Intsel Chimos SA, France, for 7-beta-hydroxy cholesteryl-3-beta-oleate for the treatment of glioma. The substance is going to be injected directly into the brain tumour contained within liposomes, which are expected to carry the medicine into the glioma cells.

HPA-23 (ammonium-21-tungsto-9- antimoniate) inhibits retrovirus replication by inhibiting RNA-dependent DNA polymerases and thus could be effective in the treatment of HIV-1 infections and AIDS. HPA-23 inhibits nucleic acid polymerases in vitro and has antiviral activity both in vitro and in vivo. Furthermore, HPA-23 inhibits HIV-1 reverse transcriptase in vitro. Inhibition occurred when treatment with HPA-23 was started 18 to 24 h after infection in the plaque assay but no effect was seen when HPA 23 was added 48 h after virus inoculation. HPA-23 was concentrated in the lysosomes and localized in the macrophages of different tissues (thymus, spleen and bone marrow). By 1986, the National Academy of Science had concluded that no therapeutic benefits for persons infected with HIV could be attributed to HPA-23. It was subsequently abandoned as a treatment option.

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.