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Palovarotene (R-667, RO-3300074) is a selective retinoic acid receptor gamma(RAR-γ) agonist for the treatment of emphysema.
Roche Holding AG is developing palovarotene (R-667, RO-3300074), a selective retinoic acid receptor gamma agonist for the treatment of emphysema. In small animal studies, palovarotene was claimed to reverse the structural, functional and inflammatory features of cigarette smoke-induced emphysema. Phase I clinical trials of palovarotene in patients with emphysema demonstrated that the drug is well tolerated, with improvements observed in markers of emphysema progression. Unlike all-trans retinoic acid, the pharmacokinetic profile of palovarotene appears to be dose-proportional. At the time of publication, a phase II, placebo-controlled trial was ongoing, and was expected to report prospective measurements of exercise, gas transfer and lung densitometry endpoints.
Palovarotene was generally well tolerated. In the study completers population, the placebo-corrected difference of lung density was -0.45 HU at week 28 (p=0.64) and -0.25 HU at week 52 (p=0.94). A nonsignificant treatment difference in most functional parameters of the lung in favour of the drug was observed over time suggesting potential pharmacological effects of palovarotene. Palovarotene 5 mg·day(-1) over 1 yr failed to show a significant benefit on lung density in moderate-to-severe emphysema secondary to severe α(1)-antitrypsin deficiency. For the detailed information of Palovarotene(R 667), the solubility of Palovarotene(R 667) in water, the solubility of Palovarotene(R 667) in DMSO, the solubility of Palovarotene(R 667) in PBS buffer, the animal experiment (test) of Palovarotene(R 667), the cell expriment (test) of Palovarotene(R 667), the in vivo, in vitro and clinical trial test of Palovarotene(R 667), the EC50, IC50,and affinity,of Palovarotene(R 667), For the detailed information of Palovarotene(R 667), the solubility of Palovarotene(R 667) in water, the solubility of Palovarotene(R 667) in DMSO, the solubility of Palovarotene(R 667) in PBS buffer, the animal experiment (test) of Palovarotene(R 667), the cell expriment (test) of Palovarotene(R 667), the in vivo, in vitro and clinical trial test of Palovarotene(R 667), the EC50, IC50,and affinity,of Palovarotene(R 667), Please contact DC Chemicals. |
