CTA002

CTA002, also known as QW1624F2-2, is a novel vitamin D analog with a dual mechanism of action. It is a strong activator of the vitamin D signaling pathway and also a potent inhibitor of CYP24 activity (the enzyme responsible for the catabolism of vitamin D; CYP24 is also a candidate oncogene). Cytochroma has shown, in both in vitro and in vivo cancer models, that CTA002 is synergistic with standard chemotherapeutics as well as, by itself, possessing anti-tumorigenic effects without causing toxicity. In vivo studies have shown that CTA002 is approximately 100-fold less calcemic than calcitriol when given orally.

Even at 28 days after the treatment ended, tumor growth suppression using the combination of CTA002 and paclitaxel was maintained at 89% compared to only 45% using paclitaxel alone (p<0.05). Equally encouraging was the observation that body weight continued to increase in the combination treatment arm and the drug regimen was well-tolerated with none of the animals demonstrating any clinically observed toxic side effects.

Selected Publication List

Reddy et al., Anticancer effects of the novel 1α,25-dihydroxyvitamin D3 analog QW1624F2-2 in human neuroblastoma. J. Cell. Biochem. 97:198-206, 2006.

Posner et al., Low-calcemic, efficacious, 1α,25-dihydroxyvitamin D3 analog QW-1624F2-2: Calcemic dose-response determination, preclinical genotoxicity testing, and revision of A-ring stereochemistry. Steroids 69:757-762, 2004.

Posner et al., Noncalcemic, antiproliferative, transcriptionally active, 24-fluorinated hybrid analogues of the hormone 1α,25-dihydroxyvitamin D3. Synthesis and preliminary biological evaluation. J. Med. Chem. 41:3008-3014, 1998.

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