AMD 3100
JM 3100, SDZ SID 791
Adis Comments
AMD 3100 (JM 3100, SDZ SID 791) is a bicyclam derivative with potent and selective activity against HIV-1 and HIV-2 in vitro and low cytotoxicity. The compound appears to act as a blocker of the CXCR4 chemokine receptor, a crucial co-factor for HIV to infect T lymphocytes. In addition, AMD 3100 appears to inhibit specific events involved in retroviral uncoating and assembly. For these reasons, AMD 3100 is considered the prototype of a new class of antiretroviral agents.
AMD 3100 was synthesised by Johnson Matthey (now Anor MED) in collaboration with the Rega Institute of Leuven, Belgium, and was under preclinical investigation with Novartis as SDZ SID 791 for the treatment of HIV infection. However, Novartis returned the rights to the compound and Anor MED has commenced a phase II study at 3 centres in the US including the Johns Hopkins University School of Medicine. This trial is expected to enrol 20 to 30 patients with HIV infection.
To date, AMD 3100 has been administered by injection in clinical studies; however, Anor MED has an active development programme for the synthesis of orally active formulations of AMD 3100 and is also developing a subcutaneous form of the drug.