FDA Approves Olysio (simeprevir) in Combination with Sofosbuvir for Genotype 1 Chronic Hepatitis C Infection

In continuation of my update on sofosbuvir

Janssen Therapeutics, Division of Janssen Products, LP (Janssen) announced the U.S. Food and Drug Administration (FDA) has approved Olysio (simeprevir), a hepatitis C virus (HCV) NS3/4A protease inhibitor, in combination withsofosbuvir as an all-oral, interferon- and ribavirin-free treatment option for genotype 1 chronic hepatitis C (CHC) infection in adult patients as part of a combination antiviral treatment regimen. Sofosbuvir is an HCV nucleotide analog NS5B polymerase inhibitor developed by Gilead Sciences, Inc.

FDA Approves Olysio (simeprevir) in Combination with Sofosbuvir for Genotype 1 Chronic Hepatitis C Infection

Active ingredient of ipecac syrup inhibits growth of cancer cells

An old home remedy called ipecac syrup, once stocked in medicine cabinets in case of accidental poisoning, is showing promise as a new chemotherapy drug for bladder cancer.

Years ago, ipecac syrup was used to induce vomiting in poisoning cases. Now a Loyola University Medical Center study has found that the active ingredient of ipecac syrup effectively inhibits the growth of bladder cancer cells, especially when combined with a standard chemotherapy drug.

In the new study, Loyola researchers exposed cell lines of normal and cancerous bladder cells to emetine alone and to emetine plus cisplatin. (Cisplatin is the standard chemotherapy drug for advanced bladder cancer.)

• Emetine alone inhibits the proliferation of bladder cancer cell lines.
• Emetine acts synergistically with cisplatin to inhibit bladder cancer proliferation better than either drug does alone.
• Emetine has little effect on normal cells.

Bladder cancer is the fourth most common cancer in men and the 9th most common cancer in women. But even with aggressive surgery and chemotherapy, the five-year survival rate for patients with advanced Stage 4 bladder cancer is only 4 to 20 percent.

"There is an urgent need to develop new drug combinations," Dr. Gupta said. "Our study demonstrates that combining emetine with cisplatin is potentially beneficial, and merits further study in clinical trials."

Dr. Gupta is an assistant professor in the departments of Urology and Surgery and in the Oncology Research Institute of Loyola University Chicago Stritch School of Medicine. Dr. Foreman is an associate professor in the Department of Pathology and the Oncology Research Institute. Other authors are John Jesse III, a Stritch student, and Paul Kuo, MD, FACS, chair of Loyola's Department of Surgery and director of the Oncology Research Institute.

Ref : http://loyolamedicine.org/newswire/news/familiar-remedy-shows-promise-new-chemo-drug-bladder-cancer

Active ingredient of ipecac syrup inhibits growth of cancer cells

Carboranes Increase the Potency of Small Molecule Inhibitors of Nicotinamide Phosphoribosyltranferase - Journal of Medicinal Chemistry (ACS Publications)

We know that,  carborane is a cluster composed of boron and carbon atoms. Like many of the related boranes, these clusters are polyhedra and are similarly classified as closo-, nido-, arachno-, hypho-, etc. based on whether they represent a complete (closo-) polyhedron, or a polyhedron that is missing one (nido-), two (arachno-), or more vertices. Interesting examples of carboranes are the extremely stable icosahedral closo-carboranes.

A prominent example is the charge-neutral C₂B₁₀H₁₂ or o-carborane with the prefix o derived from ortho, which has been explored for use in a wide range of applications from heat-resistant polymers to medical applications.  

Now researchers lead by Dr. Lee of University of Missouri used carboranes to build new drugs designed to shut off a cancer cell's energy production, which is vital for the cell's survival. All cells produce energy through complex, multi-step processes. The key to an effective drug is targeting the process that cancer cells depend on more than healthy cells. By increasing the binding strength of a drug, a smaller dose is required, minimizing side effects and increasing the effectiveness of the therapy. With carboranes, Lee found that the drug is able to bind 10 times more powerfully.

"The reason why these drugs bind stronger to their target is because carboranes exploit a unique and very strong form of hydrogen bonding, the strongest form of interactions for drugs," Lee said.

Lee said that this discovery also will lead to further uses for the drug.

"Too often, after radiation or chemotherapy, cancer cells repair themselves and reinvade the body," Lee said. "This drug not only selectively shuts off the energy production for the cancer cells, but it also inhibits the processes that allow those cancer cells to repair themselves. When we tested our carborane-based drugs, we found that they were unimaginably potent. So far, we have tested this on breast, lung and colon cancer, all with exceptional results."

According to Lee, this is the first study to show systematically how carboranes can improve the activity of a drug. Lee believes this discovery will open additional possibilities of improving drugs that are used to treat other diseases, not just cancer.

"The end result is that these new drugs could be many thousands of times more potent than the drugs that are used in the clinics today," Lee said.

 Carboranes Increase the Potency of Small Molecule Inhibitors of Nicotinamide Phosphoribosyltranferase - Journal of Medicinal Chemistry (ACS Publications)