Trimelamol (CB10-375; NSC283162) is an efficient acid-catalyzed DNA interstrand cross-linker with low neurotoxicity due to its limited penetration of the blood-brain barrier. It exhibits antitumor activity and can overcome platinum resistance. Trimelamol is utilized in research concerning lung and ovarian cancers.

Trimelamol exerts cytotoxic effects directly through its N-hydroxymethyl groups, with irreversible toxicity upon drug removal. It acts more rapidly than HMM and PMM. The primary antitumor mechanism of Trimelamol (0.5-500 μM, 1 h) involves DNA cross-linking, significantly at concentrations ≥ 2.5 μM in [32 P-end-labelled] pBR322 plasmid DNA, with higher efficiency under acidic conditions. Trimelamol shows broad-spectrum cytotoxicity and is effective against platinum-resistant ovarian cancer cells (IC 50 range: 8.5-55.4 μM).

Trimelamol, administered intraperitoneally at doses of 15-60 mg/kg daily for five times over four weeks, demonstrates efficacy in xenograft mouse models of both platinum-sensitive/resistant ovarian cancer and hormone-dependent breast cancer, with particularly notable results in acquired resistance models. Additionally, Trimelamol (7.5-60 mg/kg, i.p, once daily for five days over a three-week period) when given parenterally, shows significant effectiveness in BALB/c female mice with subcutaneously implanted T-61/MX-1 tumors, but has weaker activity against Br-10 tumors in the same mice model. While it exhibits moderate toxicity at higher doses, its toxicity is manageable at lower concentrations.