Vapitadine (R129160; Hivenyl™) is an antihistamine that Barrier Therapeutics is developing as a treatment for allergic reactions of the skin, such as those associated with hives and for the itch associated with atopic dermatitis. Vapitadine is a new selective, non-sedative H1antihistamine. In several in vitro and in vivo pharmacological models, vapitadine is at least as potent as cetirizine (Zyrtec®) and does not penetrate the blood-brain barrier. An advantage of vapitadine over other antihistamines may be the absence of the sedation, even at high doses. Vapitadine had been in phase II clinical trials for the treatment of patients with atopic dermatitis. However, no development has been reported.

Vicriviroc or SCH 417690 is a potent and selective antagonist of the CCR5 receptor. vicriviroc binds specifically to the CCR5 receptor and prevents infection of target cells by CCR5-tropic HIV-1 isolates. In antiviral assays, vicriviroc showed potent, broad-spectrum activity against genetically diverse and drug-resistant HIV-1 isolates and was consistently more active than SCH-C in inhibiting viral replication. This compound demonstrated synergistic anti-HIV activity in combination with drugs from all other classes of approved antiretrovirals. Competition binding assays revealed that vicriviroc binds with higher affinity to CCR5 than SCH-C. Functional assays, including inhibition of calcium flux, guanosine 5'-[35S]triphosphate exchange, and chemotaxis, confirmed that vicriviroc acts as a receptor antagonist by inhibiting signaling of CCR5 by chemokines. Finally, vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects. Vicriviroc represented a promising new candidate for the treatment of HIV-1 infection. Vicriviroc for HIV treatment was previously in Phase III studies but has since been discontinued.

Sotirimod is designed to treat actinic keratosis and other conditions and is a follow-up of Aldara (active substance: imiquimod). Sotirimod and imiquimod are immunomodulatory drugs that activate the body's immune system to combat skin changes such as actinic keratosis. Sotirimod is immunostimulants and Toll-like receptor 7 agonist. Sotirimod was originally developed by 3M Pharmaceuticals, then licensed to Meda in Europe for the treatment of actinic keratosis in 2007. Sotirimod had been in phase III development for the treatment of actinic keratosis. However, there is no recent development report for this study.

Etalocib (LY-293111 or VML 295) is a potent and orally active leukotriene B4 receptor antagonist of the biphenylphenol class. It efficiently blocks neutrophil activation and subsequent inflammation. Additionally, it exerts antineoplastic properties through induction of cell cycle arrest and apoptosis in tumor cells. Etalocib was being developed for the treatment of inflammatory diseases and solid tumors.

Clobenzepam (tarpane) is a drug exhibiting antihistaminic properties.

There is no information about biological and medical application of dorastine . It’s known, that compound possesses antihistamine properties and can be obtained from 4-chloroaniline.

Pirdonium is an antihistamine agent. It is the hydrophilic Histamine H1 receptor antagonist.

Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.

Methaphenilene, an antihistaminic agent, was studied as a peroxisome proliferator. Information about the current use of this compound is not available.