The novel farnesylated dibenzodiazepinone, ECO-4601 (Diazepinomicin) was discovered at Ecopia BioSciences via their novel genomics DECIPHER® platform and independently at Wyeth as an antibiotic. ECO-4601 had activity against a broad spectrum of solid tumor cell lines and was efficacious in mouse models of gliomas, prostate and breast cancers. This Micromonospora metabolite was initially produced from a strain, isolated from a Montreal soil, sporadically at < 3 μg/mL. Strain optimization led to reliable production two orders of magnitude higher. The extreme lipophilic nature and unusual solubility characteristics presented two major problems. ECO-4601 is well-soluble in only very polar organic solvents and almost insoluble in water, chlorinated solvents and hydrocarbons. Purification was initially a problem as major losses were incurred by HPLC. HSCC provided material in high yield and purity but required specialized equipment for scale up. This problem was overcome by obtaining crystals from aqueous methanol. The second problem was one of administration. ECO-4601 is soluble to ~ 5 μg/mL in physiological saline or dextrose and this was increased by 3 orders of magnitude by formulation with cyclodextrin, PEG-400 and ethanol. Mouse studies indicated that efficacy was correlated with sustained plasma levels of ≥ 2 μM. Rapid elimination (t1/2α and β in rats 4.7 min and 2.5 hr respectively) necessitated c.i.v. administration. The dose escalation portion of a Phase I trial was completed by the end of 2006 with no undue adverse effects at the highest scheduled dose, 480 mg/m²/day, and this dose was chosen for the extension portion.