IROFULVEN is a semisynthetic derivative of a natural sesquiterpene toxin illudin S, isolated from the fungus Omphalotus illudens. It alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. It requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. IROFULVEN is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and P-glycoprotein than other alkylating agents. IROFULVEN has been evaluated in 19 clinical trials, predominantly in refractory prostate and ovarian cancer patients. Results were positive, including a 10% response rate in patients with prostate cancer previously treated with docetaxel and 13% in ovarian cancer patients relapsing between 6 and 12 months after standard treatment with carboplatin and paclitaxel.

Upidosin [REC 152739, REC 22009] is an α1-blocker that was in phase II trials with Recordati in Belgium and Israel for the treatment of benign prostatic hyperplasia. When evaluated in radioligand binding assays with expressed animal or human alpha-1 ARs, Upidosin shows marked to moderate selectivity for the alpha-1a AR subtype. Its affinity for the recombinant alpha-2 AR subtypes or native dopaminergic D2 receptor was about 100-fold lower than that for alpha-1a AR subtype.

Verazide, which is related to Isoniazid has been developed in Australia for the treatment of pulmonary tuberculosis. It is equally effective as Isoniazid and less toxic.

Lexipafant is a platelet-activating factor (PAF) antagonist. It was hypothesized that the substance could beneficially affect the cognitive performance of HIV infected people. Lexipafant was as tolerable as placebo. At week 6 and week 10 after baseline evaluations, the lexipafant group showed trends toward improvement on the Rey Auditory Verbal Learning test as well as the timed gait test. A phase IIa placebo-controlled study reported that lexipafant was not effective in patients with severe ulcerative colitis receiving corticosteroids. Two lexipafant treated patient had adverse events: severe influenza-like symptoms in one and hypotension with iliac artery thrombosis in one. The clinical trials of lexipafant in the treatment of acute pancreatitis were undertaken with considerable optimism. There was a significant reduction in the incidence of organ failure and in total organ failure score at the end of medication (72 h).

Ilonidap, a tenidap derivative agent possesses an anti-inflammatory properties.

Bemoradan (RWJ-22867), a potent positive inotropic agent, inhibits cardiac phosphodiesterase fraction III. This compound was developed for the management of congestive heart failure. However, the information about the nowadays study of bemoradan is not available.

Tribuzone is a non-steroidal anti-inflammatory drug (NSAID) that has been used to treat gout and Gilbert's syndrome. The usual adverse effects of NSAIDs have been observed with tribuzone, namely gastric effects, fluid retention and headache. Like other 3-oxoalkyl substituted diphenyldioxopyrazolidines it inhibits platelet aggregation.

Trifezolac is an ibufenac derivative. It is an analgesic, antipyretic, anti-inflammatory agent.

Triclodazol is a tranquilizer.

Trimecaine is an amide series local anesthetic with antiarrhythmic activity. It was shown to be capable of eliminating the flutter of atria in dogs simulated by an electric stimulation of the myocardium and atrial fibrillation in cats induced with aconitin and precludes ventricular fibrillation in rats arising due to intoxication with calcium chloride. Trimecaine noticeably mitigates the toxic effect of strophanthin. While depressing the automatism of the sinoatrial node the drug does not affect the conduction function. The combination of epidural trimecaine with morphine after a major urological surgery provides a superior analgesia with fewer side effects when compared to epidurally delivered bupivacaine with fentanyl.