By Donald Zuhn --
OPKO Health, Inc. announced yesterday that the U.S. Patent and Trademark Office has issued U.S. Patent No. 7,345,027, which is directed to methods of inhibiting the expression of human vascular endothelial growth factor (VEGF), degrading VEGF mRNA, inhibiting angiogenesis, or treating an angiogenic disease using a specific short interfering ribonucleic acid (siRNA) molecule. While the '027 patent is assigned to the Trustees of the University of Pennsylvania, OPKO states that it has exclusively licensed the patent on a worldwide basis.
According to OPKO's statement, the '027 patent covers the Miami-based healthcare company's siRNA drug candidate, bevasiranib, which is currently in a Phase III trial for the treatment of wet age-related macular degeneration (AMD). In addition, the '027 patent covers the use of the recited siRNA molecule for treating VEGF-related angiogenic disorders such as diabetic retinopathy and cancer. OPKO Executive Vice President Samuel Reich stated that the issuance of the '027 patent "marks another important step in establishing OPKO's leadership position in the promising field of siRNA-based therapeutics," observing that "Bevasiranib was the first siRNA to enter human trials, the first siRNA to demonstrate clinically relevant activity in patients, the first siRNA to enter a Phase III pivotal trial and now, one of the first siRNAs to receive a U.S. patent covering its broad therapeutic use." OPKO's release also noted that the multi-national Phase III COBALT (Combining Bevasiranib And Lucentis Therapy) clinical trial of bevasiranib for the treatment of wet AMD is currently enrolling patients at multiple clinical sites, and that more information about the COBALT trial could be obtained here.
The '027 patent issued from U.S. Application No. 11/422,932, filed June 8, 2006, which is a divisional of U.S. Application No. 10/294,228, filed November 14, 2002, which issued as U.S. Patent No. 7,148,342, which claims the benefit of U.S. Provisional Application No. 60/398,417, filed July 24, 2002. Representative claims 1, 24, 29, and 40 of the '027 patent recite:
1. A method of inhibiting expression of human vascular endothelial growth factor (VEGF) comprising:
administering to a subject an effective amount of a short interfering ribonucleic acid (siRNA) comprising a sense RNA strand and an antisense RNA strand, wherein the sense and the antisense RNA strands form an RNA duplex, and wherein the sense RNA strand comprises a nucleotide sequence identical to a target sequence of about 19 to about 25 contiguous nucleotides in human vascular endothelial growth factor (VEGF) mRNA and wherein the sense RNA strand comprises SEQ ID NO:77, and the antisense strand comprises SEQ ID NO:78.24. A method of inhibiting angiogenesis in a subject comprising:
administering to the subject an effective amount of a short interfering ribonucleic acid (siRNA) a sense RNA strand and an antisense RNA strand, wherein the sense and the antisense RNA strands form an RNA duplex, and wherein the sense RNA strand comprises a nucleotide sequence identical to a target sequence of about 19 to about 25 contiguous nucleotides in human vascular endothelial growth factor (VEGF) mRNA and wherein the sense RNA strand comprises SEQ ID NO: 77 and the antisense strand comprises SEQ ID NO: 78.29. A method of treating an angiogenic disease in a subject comprising:
administering to a subject an effective amount of a short interfering ribonucleic acid (siRNA) comprising a sense RNA strand and an antisense RNA strand, wherein the sense and the antisense RNA strands form an RNA duplex, and wherein the sense RNA strand comprises a nucleotide sequence identical to a target sequence of about 19 to about 25 contiguous nucleotides in human vascular endothelial growth factor (VEGF) mRNA, and wherein the sense RNA strand comprises SEQ ID NO: 77 and the antisense strand comprises SEQ ID NO: 78, such that angiogenesis associated with the angiogenic disease is inhibited.40. A method of degrading human vascular endothelial growth factor (VEGF) mRNA comprising:
administering to a subject an effective amount of a short interfering ribonucleic acid (siRNA) comprising a sense RNA strand and an antisense RNA strand, wherein the sense and the antisense RNA strands form an RNA duplex, and wherein the sense RNA strand comprises a nucleotide sequence identical to a target sequence of about 19 to about 25 contiguous nucleotides in human vascular endothelial growth factor (VEGF) mRNA and wherein the sense RNA strand comprises SEQ ID NO: 77, and the antisense strand comprises SEQ ID NO: 78.
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