Moveltipril is a captopril derivative patented by Japanese pharmaceutical company Chugai Pharmaceutical Co., Ltd. as an angiotensin-converting enzyme inhibitor, that decreases systemic blood pressure more slowly and persistently than captopril. Moveltipril is partially metabolized to captopril by hydrolysis, predominantly in the liver. In preclinical studies administration of Moveltipril to the anesthetized dogs produced a gradual and dose-dependent decline in aortic pressure associated with no marked changes in coronary blood flow, heart rate. Both Moveltipril and captopril inhibited selectively the pressor response to angiotensin I in a dose-related manner.

Indolapril (CI-907) is a new orally active prodrug of nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, developed by Warner-Lambert/Parke-Davis Pharmaceutical Research for treating hypertension. Indolapril is epimer of trandolapril, well-known ACE inhibitor currently in the market for hypertension treatment. Indolapril (Monoester form) and it’s active component (diacid form) produced concentration related ACE inhibition in guinea-pig serum (IC50 for monoester -- 0.1 mkM and for diacid -- 2.6 nM). In isolated rabbit aortic rings and in rat and dog autonomic studies, Indolapril is highly specific in suppressing the contractile or pressor responses to angiotensin I. In two-kidney, one-clip Goldblatt hypertensive rats, single daily doses (0.03-30 mg/kg p.o.) produced dose-dependent decreases in blood pressure; 3 mg/kg lowered blood pressure to normotensive levels. In the spontaneously hypertensive rat, subacute administration of Indolapril produced the same decrease in blood pressure as that obtained in the renal hypertensive rat. In diuretic-pretreated renal hypertensive dogs, 10 mg/kg normalized blood pressure. For equivalent drops in blood pressure, heart rate increases were less in Indolapril than in enalapril-treated renal hypertensive dogs. No side effects were observed with CI-907 in any of the conscious animals. The antihypertensive response to Indolapril (0.03-1.0 mg/kg p.o.) was found to correlate with inhibition of vascular tissue ACE, but not plasma or brain ACE in two-kidney, one-clip renal hypertensive rats.

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.

Flosfluridine tidoxil, a thymidylate synthase inhibitor that was developed for the treatment of actinic keratosis and solid tumors, e.g. breast and colorectal cancers. These studies were suspended and information about the further development of this drug is not available.

Epinine or deoxyepinephrine is an active form of Ibopamine, which is used as a cardiovascular agent in congestive heart failure. Epinine is a stimulant of alpha-adrenoceptor activities: alpha-1 and alpha-2. Experiments on pig’s eyes have shown that epinine can be a promising candidate substance for intraoperative (e.g., cataract surgery) intracameral use in humans.

Censavudine (also known as BMS-986001) is thymidine analogue and nucleosidereverse transcriptase inhibitors developed by Bristol Myers-Squibb for the treatment of HIV infection. In single-cycle assays, Censavudine inhibited HIV-2 isolates from treatment-naive individuals, with 50% effective concentrations (EC50s) ranging from 30 to 81 nM. Censavudine is the first nucleoside analog that, when tested against a diverse collection of HIV-1 and HIV-2 isolates, exhibits more potent activity against HIV-2 than against HIV-1 in culture. In clinical trials Censavudine was generally well tolerated through week 48 and similar efficacy to that of tenofovir disoproxil fumarate

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.

Dasolampanel (NGX-426) is an orally available competitive antagonist of the AMPA and kainate receptors. The dug originated at Eli Lilly and Horizon Pharma and was developed for the treatment of migraine and neuropathic pain. Dasalompanel was reduced capsaicin-induced pain and hyperalgesia in human volunteers but failed to achieve positive results in phase 2 clinical trials in patients with pain due to osteoarthritis of the knee and diabetic peripheral neuropathic pain.

Besifovir (also known as LB80331), an active metabolite of LB80380 was studied for the treatment of hepatitis B.