Burixafor is an orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Burixafor binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation; this may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the blood. CXC motif chemokine receptor 4 (CXCR4) blockade is pursued as an alternative to mesenchymal stem cell treatment after heart transplantation. The augmentation of conventional mycophenolate mofetil plus corticosteroids with a CXCR4 antagonist is potentially effective in improving outcomes after heart transplantation in humans

Tiprinast (MJ 12175) is one of a series of thienopyrimidine-carboxylic acids synthesized as possible antiallergy compounds. In clinical studies it has been shown to be efficacious in preventing the symptoms of ragweed hay fever when used as a nasal spray. Tiprinast has been shown to resemble disodium cromoglycate (cromolyn) in biologic activity in a variety of antigen-induced allergic test systems. Both compounds inhibit passive cutaneous anaphylaxis in the rat, histamine release from rat peritoneal mast cells and nasal constriction due to antigen in the rat. In all cases tiprinast is more potent than cromolyn and also longer acting. Tiprinast, like cromolyn, appears to elicit a cardiac reflex (Bezold-Jarisch) in the anesthetized dog.

Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.

Trenizine is a diphenylmethyl piperazine derivative. It is a vasodilator, antiemetic, antihistamine and anti-anaphylactic agent.

Rabeximod is an indolo[2,3-b]quinoxaline derivative patented by OxyPharma AB as anti-inflammatory agent useful for the treatment of autoimmune disease. Rabeximod impaired monocyte differentiation into monocyte-derived dendritic cells and pro-inflammatory allostimulated macrophages. Monocyte-derived dendritic cells that were treated with Rabeximod resulted in a significant decrease in their ability to pinocytose antigens, while no effect was exerted by the drug on the ability of allostimulated macrophages and anti-inflammatory macrophages to phagocytose. Rabeximod reduces the severity of arthritis in rodent models of rheumatoid arthritis and multiple sclerosis. Rabeximod efficiently prevented arthritis during the time window when TLR2 or TLR4 ligands activate inflammatory macrophages.

Alethine (Beta alethine) is an immunostimulant agent. It was undergoing clinical development with LifeTime Pharmaceuticals for the treatment of haematological malignancies. It is a low molecular weight disulfide that has been shown to exhibit in vivo antitumor activity in murine myeloma and melanoma models.

Tilomisole (also known as Wy-18,251) is a benzimidazole derivative patented by American Home Products Corp. as an antineoplastic agent with immunomodulating and antimetastatic activity. Tilomisole significantly enhanced the blastogenic response of cancer patients' lymphocytes in vitro. Tilomisole significantly increases macrophage phagocytosis against 51chromium labeled opsonized chicken red blood cells. In preclinical models, Tilomisole administration significantly increases peripheral blood lymphocytes in rats and demonstrates marked anti-inflammatory activity. The acute anti-inflammatory of Tilomisole.) was similar to aspirin, but in contrast to aspirin, Tilomisole failed to demonstrate antipyretic activity. Tilomisole also inhibited chronic inflammatory responses in the adjuvant- and collagen-induced arthritis models. Unfortunately, in clinical trials, Tilomisole failed to demonstrate significant antitumor responses.

Metenkephalin (Met-enkephalin) is an endogenous opioid peptide that acts as an agonist at μ-opioid receptors (μORs) and δ-opioid receptors (δORs). Met-enkephalin exhibits neuromodulatory, antinociceptive/analgesic, antidepressant, and gastrointestinal motility modulating activities. Like other endogenous opioids, met-enkephalin modulates expression of opioid receptors and plays a role in reward/reinforcement signaling. Met-enkephalin is also involved in exercise-induced reversal of neuropathic pain and in animals undergoing the forced swim test, decreases immobility time. Met-enkephalin inhibits gastrointestinal muscle contractility, inhibiting motility and gastric emptying. Additionally, analogs of this peptide display anticancer and antiepileptic/anticonvulsant activities.