Therapeutics

CINV

Rolapitant

Rolapitant is potentially a best-in-class supportive care product for Chemotherapy-induced nausea and vomiting (CINV). Characteristics include:

  • Single dose
  • Rapid onset
  • Long-acting (5 day activity as opposed to 1 or 2 days for other treatments)

Acquisition of Rolapitant

  • In October 2009, OPKO acquired Rolapitant, a potent and selective competitive antagonist of the NK-1 receptor, in addition to other neurokinin-1 (NK-1) assets from Schering Plough Corporation.
  • In December 2010, OPKO exclusively out-licensed the development, manufacture, and commercialization of Rolapitant to biopharmaceutical company TESARO, Inc.

Clinical Development

Rolapitant has completed Phase 3 clinical development for CINV. Two phase 3 trials of rolapitant that together enrolled a total of 1,070 patients receiving highly emetogenic chemotherapy (HEC) and met the primary endpoint of a higher rate of complete response in the delayed phase. The results indicated that protection from CINV was maintained over the full five day at-risk period in both trials. One additional phase 3 trial of rolapitant that enrolled 1,369 patients receiving moderately emetogenic chemotherapy (MEC) successfully achieved the primary endpoint of higher rate of complete response in the delayed phase. a New Drug Application (NDA) is on track for mid-2014.

License Agreement with TESARO

  • Under terms of the license with TESARO, OPKO is eligible to receive up-front and milestone payments of up to $121 million.
  • OPKO is also entitled to double-digit tiered royalties on sales of the licensed product, a share of future profits from product commercialization in Japan, and an option to market the product in Latin America.
  • OPKO has also acquired an equity position in TESARO.

Market Opportunity

  • U.S. market opportunity of approximately $1.25 billion
  • 6.6 million annual CINV patient treatments in 2011
  • NCCN and ASCO guideline recommendations could lead to 70% penetration by the NK-1 class
  • Merck-EMEND®  is currently the only NK-1 receptor antagonist on the market
  • Strong IP portfolio with U.S. exclusivity expected through 2028