Lupeol, a biologically active dietary triterpenoid, is found in many medicinal plants and different fruits such as olives, mangos, and strawberries. Lupeol exhibits a wide spectrum of pharmacological properties including anti-inflammatory, anti-cancer, anti-diabetic, anti-microbial, cardioprotective, and hepatoprotective activities. Lupeol inhibits LPS-induced microglial neuroinflammation via the P38-MAPK and JNK pathways and has therapeutic potential to treat various neuroinflammatory disorders. Lupeol possesses antiskin tumor-promoting effects in CD-1 mouse and inhibits conventional as well as novel biomarkers of tumor promotion. It strongly suppressed lipogenesis by modulating the IGF-1R/phosphatidylinositide 3 kinase (PI3K)/Akt/sterol response element-binding protein-1 (SREBP-1) signaling pathway in SEB-1 sebocytes, and reduced inflammation by suppressing the NF-κB pathway in SEB-1 sebocytes and HaCaT keratinocytes. Lupeol exhibited a marginal effect on cell viability and may have modulated dyskeratosis of the epidermis. These results demonstrate the clinical feasibility of applying lupeol for the treatment of acne.

Setrobuvir (also known as ANA-598 and RG7790) is an orally administered, small-molecule non-nucleoside polymerase inhibitor, which was in development by Roche company. Setrobuvir has been used in trials studying the treatment of chronic hepatitis C. Setrobuvir is a non–nucleoside NS5B inhibitor (NNI). It has shown potency and a high degree of specificity against HCV genotype 1 NS5B polymerase, leading to 73% SVR when orally administrated to patients in combination with pegylated interferon and ribavirin. An interferon-free setrobuvir based regimes of three direct acting antivirals (DAAs) plus ribavirin has also been shown to be safe and effective in genotype 1 treatment naive patients.

Brilacidin (formerly PMX-30063) is a polymer-based antibiotic and an investigational new drug, that was studied in human clinical trials, and represents a new class of antibiotics called host defense protein mimetics. Brilacidin is an antibiotic that works by disrupting bacterial cell membranes, mimicking defensins that play a role in innate immunity. Brilacidin has shown great efficacy in phase II clinical trials against acute Staphylococcus aureus skin and skin structure infections, comparable to that of the lipopeptidic drug daptomycin, which is currently used clinically to treat drug-resistant staph infections. Brilacidin also has potent broad-spectrum activity in vitro against several other Gram-positive and Gram-negative pathogenic bacteria, including several multidrug-resistant strains.

IPI-493 (17-AG, 17-Aminogeldanamycin) is the major metabolite of tanespimycin (17-AAG) and retaspimycin (17-DMAG) with potent antineoplastic activity. Hsp90 controls the proper folding, function, and stability of various "client" proteins within cells. Many of the clients of Hsp90 (such as Akt, Bcr-Abl, EGFR, Flt-3, c-Kit and PDGFR α) are oncoproteins or important cell-signaling proteins, and therefore are critical for tumor cell growth and survival. Inhibition of Hsp90 results in degradation of these proteins, which abrogates growth and survival signaling and leads to tumor cell death. IPI-493 has been used in trials studying the treatment of Advanced Malignancies.

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.

Ordopidine (also known as ACR-325) is a dopaminergic stabilizer that acts as dopamine D2 receptor antagonists with low affinity. Ordopidine under the development of NeuroSearch participated in phase I trials for the treatment of Parkinson's disease and bipolar disorder. Information about the current study of this drug is not available.

Bisegliptin (also known as KRP-104) was developed as an orally active dipeptidyl peptidase IV (DPPIV) inhibitor. It is known, that DPPIV inhibition reduces blood glucose through suppression of the degradation of the insulin-releasing hormone. Bisegliptin successfully completed the phase II clinical trials for patients with type 2 diabetes. However, further development of the drug has been discontinued for business reason. The company wasn’t able to find a tie-up partner to co-develop.