Napirimus is an immunosuppressant agent.

Ancriviroc (SCH 351125) is a small-molecule antagonist of the human immunodeficiency virus type 1(HIV-1) coreceptor CCR5. It has in vitro activity against R5 viruses with 50% inhibitory concentrations ranging from 1.0 to 30.9 nM. Ancriviroc is an orally bioavailable small molecule inhibitor of HIV-1 entry via CCR5 coreceptor interaction. Ancriviroc has potent activity against RANTES binding (K(i) = 2 nM), possesses subnanomolar activity in blocking viral entry and has excellent antiviral potency versus a panel of primary HIV-1 viral isolates. Ancriviroc had been in phase I clinical trials by Schering-Plough (subsidiary of Merck Sharp & Dohme) for the treatment of HIV infection. However, this research has been discontinued.

Ammonium trichlorotellurate (AS-101) is a synthetic non-toxic tellurium derivative, structurally similar to cisplatin, with immunostimulatory and anti-hair loss properties. Ammonium trichlorotellurate induces production of colony stimulating factor (CSF), interleukin-2 (IL-2), and IL-2 receptors by increasing the calcium ion influx through the cell membrane and subsequently exerts its immunostimulatory effects through the CSF-mediated increase in macrophage/granulocytes. This agent is also a potent inducer of interferon and a spectrum of cytokines such as IL-1, IL-6, and tumor necrosis factor (TNF). In animal studies, ammonium trichlorotellurate exerts its anti-hair loss effect by inducing anagen and obstructing spontaneous catagen via promoting follicular keratinocyte proliferation and interfering with terminal differentiation, respectively. AS-101 suppresses production of HIV-1. It inhibited reverse transcriptase activity and replication of human immunodeficiency virus type 1. RDDP and DDDP activities were impaired by the drug with calculated IC50 value of about 4 uM. Intravenous AS-101 was in trials in patients with HIV infections. AS-101, a small-molecule integrin αvβ3 and VLA-4 inhibitor is being developed by BioMAS in Israel for the treatment of genital warts, age-related macular degeneration and fertility preservation. Phase II clinical trials are ongoing. The drug was also undergoing phase II development in acute myeloid leukaemia, atopic dermatitis, chemotherapy-induced damage, myelodysplastic syndromes, thrombocytopenia, alopecia, psoriasis. However, development for these indications was discontinued.

Temurtide was developed as an immune adjuvant. Information about the current application of this drug is not available.

Elbanizine [HWA 214] is an antihistamine which was undergoing preclinical trials with Hoechst Marion Roussel in Germany for the treatment of allergic asthma. Elbanizine does not have such drawbacks as causing drowsiness or being effective only as a prophylactic drug, and could provide advantages over other non-sedative compounds, such as terfenadine and astemizole, in that it is water soluble and thus can be administered through inhalation or through intravenous application.

Pibaxizine is diphenylmethyl piperazine derivatives. It is a histamine H1 receptor antagonist. Animal experiments have shown that it has spasmolytic properties for smooth muscle, particularly in the bronchi, as well as anticholinergic and anti-serotonin activities. It can be concluded that Pibaxizine has a strong protective effect against bronchospasm caused by inhalation of a histamine aerosol. Protection against methacholine-induced bronchospasm was less marked. Pibaxizine had been in phase II clinical trial for the treatment of chronic obstructive pulmonary disease. However, this development was discontinued.

Prospidium is a diazoniadispiro(5.2.5.2)hexadecane derivative patented by All-Union Scientific-Research Chemical-Pharmaceutical Institute as an antitumor agent that does not inhibit hematopoiesis. In preclinical models, The injection of Prospidium to thyroidectomized and hypophysectomized rats inhibited tumor growth to a greater extent than in intact rats. Larynx and lung cancer, lymphogranulomatosis, leucosis, etc. can be successfully treated with Prospidium at doses of 60-120 mg daily.

Tresperimus is a new stable immunosuppressive analog of 15-deoxyspergualin (DSG) obtained by organic chemical synthesis. It was initially developed as an antitumor agent. Tresperimus has been designed to be chemically stable in aqueous solution. Tresperimus controlled alloreactivity in a fully major histocompatibility complex (MHC) mismatched rat cardiac transplant model and also induced donor-specific long-lasting unresponsiveness. Posttransplant tresperimus therapy effectively protected mice from lethal graft-versus-host disease (GVHD) in a dose-related manner. It has been shown to suppress graft rejection as efficiently as cyclosporine A. Indeed, a short course of tresperimus has similar or better effects compared to the effects of cyclosporine in bone marrow, cardiac, and skin transplant models. Prevention of rejection is related to the induction of donor-specific tolerance without affecting immunity to third-party antigens. In addition, CD4+ T-cells from tresperimus-treated animals can transfer donorspecific tolerance to naive animals, an effect not seen with cyclosporine or other traditional immunosuppressive drugs. The mechanism by which tolerance is induced is not clear. Tresperimus binds to Hsc70, a heat shock protein– chaperoned peptide that, among other effects, inhibits nuclear localization of nuclear factor (NF)-kB, which is required for CD40 and CD28 ligation signaling in antigen-presenting cells, an important early step in T-cell costimulation. Locally administered tresperimus appears to be a potential immunosuppressive agent in the management of intraocular inflammation. Tresperimus had been in phase III clinical trial for the treatment of graft-versus-host disease. However, this development was discontinued.

Icotidine (also known as SKF 93319) was developed as histamine H1- and H2-receptor antagonist and possessed antinociception properties. Due to its antagonist activity, was suggested that compound could have therapeutic in some inflammatory skin diseases such as the urticarias and mastocytosis.