Gadocoletic acid (also Gadoletic acid trisodium salt, or B22956/1) is a magnetic resonance contrast agent. Based on results from animal imaging experiments and pharmacokinetic data it was suggested that gadocoletic acid trisodium salt has strong potential for clinical use in Magnetic Resonance Coronary Angiography and Myocardial Perfusion Imaging. The small molecules of gadocoletic acid are bound after injection to large human serum albumin molecules in coronary vessels with the result of high vessel/muscle contrast. The ability of B229563− (anion) to bind to more than one site on the albumin molecule allows a positive correlation between dose and blood relaxation rate enhancement at doses higher than 0.05 mmol/kg, the dose that produces roughly a total plasma concentration equimolar to the albumin concentration at equilibrium distribution. Gadocoletic acid is thought to be highly efficacious in inversion recovery-prepared 3D gradient-recalled echo, navigator echo-gated coronary angiography in humans already at doses below 0.1 mmol/kg.

Peldesine (also known as BCX-34) was developed as a purine nucleoside phosphorylase (PNP) inhibitor. It is known PNP inhibitors may be useful for treating a variety of T-cell related autoimmune diseases including psoriasis, rheumatoid arthritis, and Crohn s disease and T-cell cancers. Peldesine has undergone phase I trials for the treatment of human Immunodeficiency virus (HIV) infections. In addition, this drug participated in phase III clinical trial as a topical therapy for cutaneous T-cell lymphoma. This drug was also studied as a potential therapy for psoriasis, multiple sclerosis; rheumatoid arthritis; transplant rejection. However, all these indications were discontinued because of the lack of significant effects over placebo.

BMS-906024 is a lead candidate of a series of inhibitors of gamma secretase-mediated Notch signalling. BMS-906024 is an orally bioavailable, small-molecule gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor BMS-906024 binds to GS and blocks activation of Notch receptors, which may inhibit the proliferation of tumor cells with an overly-active Notch pathway. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains that lead to their activation. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth. BMS-906024 is currently in Phase 1 clinical trials for patients with T-cell acute lymphoblastic leukemia and metastatic solid tumors, including lung cancer.

Sodium aceneuramate is a sodium salt of aceneuramic acid (sialic acid). It is an effective inhalant expectorant. Inhalation of sodium aceneuramate repaired inflammation in the airway, and caused bronchitic rabbits to produce sputa with a low viscosity, similar to normal air-way secretions. Sodium aceneuramate protected the mucociliary transport impaired bycigarette smoke in a dose-dependent manner. The results suggest that sodium aceneuramate may participate in the defense mechanism in the airway against irritant gases. Sodium aceneuramate inhibited bronchial anaphylaxis and the release of histamine into bronchoalveolar lavages. Sodium aceneuramate has an action which elevates the viscoelasticity of secretions in the respiratory tract.

METHYLENETETRAHYDROFOLIC ACID, L-(+), an endogenous biomodulator that was developed under the brand name modufolin or arfolitixorin by the Isofol Medical. Arfolitixorin is developed to increase the efficacy of standard of care chemotherapy for advanced colorectal cancer. This drug is currently being studied in a global phase 3 clinical trial. Besides, the drug successfully completed phase II as rescue therapy for osteosarcoma. 21 May 2019 Isofol Medical has received clinical patent protection for the arfolitixorinin USA. It relates to a method of increasing blood concentration of deoxyuridine, a blood biomarker for inhibition of tumor growth in human cancer treatment.

Telmapitant, a neurokinin NK1 antagonist, was developed as an anti-emetic agent that has never been marketed. Information about the current use of the telmapitant is not available.

9cUAB30 is a synthetic analog of 9-cis-RA with little or no RAR-binding activity relative to 9-cis-RA and other RA. 9cUAB30, is a selective rexinoid for the retinoid X nuclear receptors (RXR). Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells. 9cUAB30 displays substantial chemopreventive capacity with little toxicity and is being translated to the clinic as a novel cancer prevention agent. 9cUAB30 has been assessed in vitro with human cell cultures. Human hepatocytes demonstrated no signs of cytotoxicity with treatment of 9cUAB30 up to 50 umol/L, although when human breast cancer cells were treated with 9cUAB30, they showed a significant inhibition of cell proliferation and apoptotic levels 2.5to 3.5 times the levels of untreated cells. 9cUAB30 inhibits telomerase and induces apoptosis in HL60 cells.

Lobucavir is a new anti-cytomegalovirus infection agent, manufactered by Bristol Myers Squibb, Inc. Lobucavir is a cyclobutyl analog of guanine with broad spectrum antiviral activity against most herpes viruses and Hepatitis B. Lobucavir was shown to inhibit herpes simplex virus (HSV) DNA polymerase after phosphorylation by the HSV thymidine kinase. The drug was well tolerated with few side effects. Lobucavir had been in phase III clinical trial for the treatment of Hepatitis B, Herpes simplex virus infections and in phase II for the treatment of Cytomegalovirus infections. All these studies were discontinued.