Efaroxan (RX 821037) is a potent and selective alpha(2)-adrenoceptor antagonist. Additionally, Efaroxan is a selective antagonist at the imidazoline I1 receptor. Efaroxan promotes insulin secretion, in the absence of exogenous agonists, by a mechanism that involves inhibition of ATP-regulated K+ channels. Efaroxan was in clinical trials for the treatment of diabetes mellitus however its development has been discontinued.

MIV-150 is a tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2. MIV-150 has been shown to inactivate viruses that are resistant to other antiviral drugs, including non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, and protease inhibitors. MIV-150 effectively inactivated free virus. Combination of MIV-150 and Carraguard demonstrated an additive antiviral effect. Seminal fluid had no effect on the antiviral activity of MIV-150 or Carraguard. The average concentration that blocks 50% of infection (EC50) for PC-815 was approximately 10 times stronger than Carraguard for the different clinical isolates used in the study.

Meisoindigo ((E)-1,1'-dimethyl-[3,3'-biindolinylidene]-2,2'-dione) is a derivative of Indigo Naturalis, that has been used in China for chronic myeloid leukemia. In vitro cell line studies have shown that this agent might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML). Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In phase III clinical trial of Meisoindigo involving 402 patients, it was shown that Meisoindigo was equally efficient for both newly diagnosed and previously treated CML patients after oral administration. The hematological complete response (CR) and partial response (PR) rates, respectively, were 45.0 and 39.3% for newly diagnosed patients and 35.9 and 41.4% for previously treated patients. Meisoindigo was generally well tolerated. The most frequent side‑effects were bone, joint and/or muscle pain of varying degrees when the dosage was more than the suitable one.