Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.

Dacinostat (also known as LAQ824), is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. Dacinostat inhibits histone deacetylase enzymatic activities in vitro and transcriptionally activated the p21 promoter in reporter gene assays. Tumor cells treated with Dacinostat caused acetylation of HSP90 and degradation of its cargo oncoproteins. Flow cytometry studies revealed that both tumor cell lines and normal diploid fibroblasts arrested in the G2/M phase of the cell cycle after Dacinostat treatment. However, an increased sub-G1 population at 48 h (reminiscent of apoptotic cells) was only observed in the cancer cell lines treated with Dacinostat. Dacinostat exhibited antitumor effects in a xenograft animal models. In phase I trials, Dacinostat was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition. In another phase 1 in patients with advanced solid tumors, grade 3 or 4 toxicities were observed. Dacinostat had been in phase II clinical trials by Novartis for the treatment of solid tumors but further studies were discontinued.

Cinperene is an investigational compound proposed for clinical use as a strong and long-acting peripheral central anticholinergic. In animal models, cinperene inhibited mydriasis, pilocarpine-induced salivation, and lacrimation, scratching, hunching and other symptoms.

Mapracorat (BAY-865319, BOL-303242-X or ZK-245186) is a selective non-steroid glucocorticoid receptor agonist exerting anti-inflammatory activity. Mapracorat showed partial attenuation of the classical NF-κB pathway, consistent with traditional steroids. However, mapracorat uniquely potentiated a novel anti-inflammatory mechanism through rapid upregulation of RelB, an anti-inflammatory member of the NF-κB alternative pathway. Mapracorat was being studied in the treatment of ocular and skin inflammatory diseases.

Pibrozelesin (KW-2189) is a semisynthetic water-soluble derivative of the antineoplastic antibiotic duocarmycin B2. Activated by carboxyl esterase, pibrozelesin alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis. KW-2189 induced DNA strand breaks in H69 cells in a concentration-dependent manner. DNA cleavage is one of the major mechanisms of KW-2189-mediated cytotoxicity. KW-2189 showed evidence of anti-tumor activity in hepatocellular carcinoma (HCC). However, because of significant and prolonged hematologic toxicity, when given as a single dose every 6 weeks, further development of this drug in HCC is not possible. Pibrozelesin had been in phase II clinical trial for the treatment of advanced malignant melanoma and advanced renal cell carcinoma. No activity in metastatic renal cell carcinoma was demonstrated and the lack of significant antitumor activity in advanced malignant melanoma treatment was shown.

Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.

Plinabulin (formerly known as NPI-2358) is a potent microtubule-destabilizing agent that exerts its effect by binding to the colchicine-binding site of tubulin. Plinabulin projects its potent antitumor activity against a broad spectrum of tumor cell lines. This drug in combination with docetaxel is under development by BeyondSpring Pharmaceuticals in a worldwide Phase 3 clinical trial for non-small cell lung cancer. Pegfilgrastim is also in phase II clinical trial for the prevention of chemotherapy-induced neutropenia, where docetaxel, doxorubicin, and cyclophosphamide (TAC) were used as the chemotherapy. Plinabulin also possessed antitumor activity in animal models with multiple myeloma cancer cells, where the JNK protein appeared to be a primary target of plinabulin.

Spirotriazine is a dihydrotriazine derivative patented by Burroughs Wellcome & Co. (U.S.A.) Inc. as the anthelmintic agent. In preclinical models, Spirotriazine shows potent activity against intestinal parasites and negligible microbiological activity.

Ciproquazone (SL-573) is a non-steroidal anti-inflammatory drug, a derivative of quinazolinone, discovered by Sumimoto Chemical Co. in the late 1970s. Ciproquazone acts as a reversible inhibitor of prostaglandin synthetase. In animal models, ciproquazone demonstrated antipyretic, analgesic and anti-inflammatory activity. The drug was evaluated in a clinical in acute purulent diseases in the field of orodental surgery.

Pytamine is a nitrosamine derivative patented by Hercules Powder Co. as antioxidants, stabilizers, rubber additives, insecticides, fungicides, bactericides, and pharmaceutical intermediates. In preclinical trials Pytamine shows potent psychotropic effects associated modulation of GABAA receptors.