Gentamicin C2 together with epimer C2a is a part of the antibiotic of the aminoglycoside group, gentamicin. Gentamicin C2 has a methyl group in the 6′ position. Gentamicin is a broad-spectrum antibiotic that binds to the prokaryotic ribosome, inhibiting protein synthesis in susceptible bacteria. Gentamicin is bactericidal in vitro against Gram-positive and Gram-negative bacteria.

Monomethyl Auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerization of tubulin. Monomethyl Auristatin E is the synthetic analog of the antineoplastic natural product Dolastatin 10, cannot be used as a drug itself. Monomethyl Auristatin E is commonly conjugated with monoclonal antibodies directed at antigens specific to cancer cells for tumor-directed cytotoxicity. MMAE is typically coupled to the antibody via a protease-cleavable linker, allowing separation of the drug from the antibody following intracellular localization. When coupled to cAC10, Monomethyl Auristatin E shows selective cytotoxicity in CD30+ cells and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. When coupled to the anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. When coupled to the anti-HER2 antibody, pertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. In the Karpas 299 ALCL model, cAC10-vcMMAE induces complete, durable tumor regression, while free MMAE doesn’t produce detectable antitumor activity. In mouse xenograft models of NHL, anti–CD79b-vcMMAE strikingly results in sustained complete tumor remission.

Fluasterone is a fluorinated derivative of an endogenous steroid hormone androstenolone (dehydroepiandrosterone, DHEA). According to in vivo studies, fluasterone possess endocrinologic effects manifested in increased estrous cycle length and decreased the weights of the uterus, prostate, seminal vesicles, and testes. The mechanism of action of fluasterone is not yet fully elucidated, but most likely involve inhibition of glucose-6-phosphate hydrogenase. Fluasterone was developed by Aeson Therapeutics and was investigated in the late 1990s for the treatment of asthma, cancer, cardiovascular and metabolic disorders. The development of fluasterone for discontinued, probably due to a combination of low potency and insufficient oral bioavailability. Later, the development of fluasterone was continued by the company SteroTherapeutics. In 2018 the FDA has granted an orphan drug designation for fluasterone for the treatment of nonalcoholic fatty liver disease, nonalcoholic steatosis, and hyperglycemia in patients with Cushing’s syndrome.

Isobutyramide (VX-366) is an orally available branched chain amide that may offer an alternative to current treatments for beta-hemoglobinopathy. Isobutyramide has been shown to increase fetal hemoglobin (HbF) in patients with beta-hemoglobinopathies. Isobutyramide was originated at the Children's Hospital Oakland Research Institute which, in 1993, granted exclusive worldwide rights for the agent to Vertex. However, development of Isobutyramide has been discontinued for sickle cell anaemia and thalassaemia.

SC-41930 has been shown to be a specific LTB4 receptor antagonist both in vitro and in vivo. SC-41930 can produce significant anti-inflammatory effects. The anti-inflammatory activity of SC-41930 could be attributed to postreceptor inhibition of inflammatory mediator production by human neutrophil and other cells in addition to antagonism of human neutrophil LTB4 receptors.

Gossypol is a substance that is found in the cotton plant. It is removed from the seeds and used for medicine. Gossypol is effective as a nonhormonal male contraceptive; however, it has been documented to have irreversible effects on male fertility. Gossypol is reported to exhibit antioxidant, anticancer, antivirus, antiparasitic, and antimicrobial properties and lower plasma cholesterol. Nausea, emesis, anorexia, diarrhea, altered taste sensation, small intestine obstruction, and fatigue have been recorded in clinical trials as adverse reactions. Large amounts of gossypol can decrease potassium levels in the body. Low potassium levels can increase the side effects of digoxin.

DMP-777 (also termed L-694458) a cell permeant b-lactam inhibitor of a human leukocyte elastase was developed for treatment cystic fibrosis, juvenile rheumatoid arthritis.

Leupeptin is produced by various species of Actinomycetes. It strongly inhibits proteolysis by plasmin, trypsin and papin. Leupeptin is well absorbed through oral route. Leupeptin has been known to cause various neuropathological changes in vivo resembling those of aging or neurodegenerative processes in the human brain, including the accumulation of neuronal processes and neuronal cytoskeletal abnormalities leading to neurofibrillary tangle (NFT)-like formations. In in vitro experiments, leupeptin protects the heart from myocardial stunning. Leupeptin was found to inhibit tumorigenesis in mouse skin induced by a single, noncarcinogenic dose of 7,12- dimethylbenz(a)anthracene followed by repeated application of croton oil. Tumors that had already been induced were scarcely affected by leupeptin.