Pyroxamine (also known as AHR 224) is benzhydryl ethers of 3-pyrrolidinol patented by A. H. Robins Co., Inc. as antihistamine with bronchodilation activity. In preclinical studies, Pyroxamine shows moderate inhibition of histamine-induced ulceration in guinea pigs

Iomethin I-131 is radioiodinated quinoline derivative with potential tumor localizing activity. In animal models, Iomethin I-131 administrations lead to regression of the malignant melanoma and its metastases.

Imanixil (also known as HOE-402) was developed as a potent cholesterol-lowering compound, which inhibits VLDL production, and consequently attenuates atherosclerosis development. This drug participated in phase I clinical trial for the treatment of hyperlipidemia, however, this study was discontinued.

Dimetamfetamine is the N-methylated analog of methamphetamine, produces behavioral effects that are generally comparable to those of methamphetamine, but with reduced potency. It is often found as an impurity in preparations of methamphetamine. Dimetamfetamine itself is less neurotoxic than methamphetamine. Dimetamfetamine is metabolized to p-hydroxyl methamphetamine, p-hydroxyl dimetamfetamine, amphetamine, methamphetamine, and N,N-dimethylamphetamine N-oxide in humans, and flavin-containing monooxygenase-1 and CYP2D6 are mainly involved in the N-oxidation and N-demethylation of dimetamfetamine, respectively. Dimetamfetamine has also been used illegally in Korea, and the Korean government placed DMA on the official list of controlled substances on December 4, 2006.

Loxoribine [RWJ 217C7] is an immunostimulant which was developed by Johnson and Johnson. It is a selective agonist for TLR7 (Toll-like receptor 7), which possesses antitumor and antiviral properties and was investigated in a rat model of endometriosis and in addition, in phase I of a clinical trial for patients with advanced cancer.

Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.

LAROTAXEL is a taxoid with potential antineoplastic activity. It prevents microtubule depolymerization, thereby inhibiting cell proliferation. It displays a broad spectrum of antitumor activity in vitro and in vivo, including activity against P-glycoprotein expressing tumors. LAROTAXEL was in phase III clinical trials for the treatment of breast cancer, pancreatic cancer, and bladder cancer. However, its development was discontinued.

Azepexole (or previously known as B-HT 933), a selective alpha 2-adrenoceptor agonist that was studied for the man with physiological tremor. It was shown that the drug produced sedation compared to placebo but not when compared to pre-treatment values. Some studies also have revealed the anti-tussive and antihypertensive properties of azepexole.

Urefibrate, clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is an antihyperlipidaemic agent.

Atromepine (wider known as levomepate) is a levo isomer of tropine α-methyltropate. Experiments on animals have shown that this compound had marked anticholinergic action, possessed ganglionic-blocking activity and didn’t have any pathologic damages or teratogenic effects.