Navigation Links
Reformulated imatinib eliminates morphine tolerance in lab studies
Date:2/21/2012

HOUSTON By reformulating the common cancer drug imatinib (Gleevec), researchers have eliminated morphine tolerance in rats an important step toward improving the effectiveness of chronic pain management in patients, according to researchers at The University of Texas MD Anderson Cancer Center.

Narcotics such as morphine are a mainstay of chronic pain treatment. Over time, tolerance to the pain-relieving effects of these drugs can develop, requiring increasing doses to control pain. In some cases, narcotics become ineffective. This study, published online in Nature Medicine, is the first to identify a cellular signal that selectively causes narcotic tolerance.

"By suggesting a way to prevent or reverse tolerance in patients, this study could have far-reaching implications for many people suffering with chronic intractable pain," said senior author Howard B. Gutstein, M.D., professor in the Departments of Anesthesiology/Perioperative Medicine and Biochemistry at MD Anderson.

One imatinib target causes morphine tolerance

In the study, scientists discovered that activating the - isoform of the platelet-derived growth factor receptor (PDGFR) caused morphine tolerance in animals not previously exposed to morphine.

Imatinib is commonly used to treat certain types of leukemia and gastrointestinal tumors. It targets a number of cellular receptors, including the PDGFR, which is heavily expressed in those cancer cells.

In this study, imatinib prevented morphine tolerance, and importantly, completely reversed tolerance in rats that received high morphine doses continuously for several days, which reflects how morphine and other opioids are often given to chronic pain patients.

Researchers modify imatinib to block PDGFR

Morphine and other opioids work by binding to mu opioid receptorsin the brain and spinal cord.

Imatinib's ability to inhibit morphine tolerance has not yet been observed in cancer patients who take imatinib because the drug does not penetrate the nervous system. Gutstein's group reformulated imatinib using a simple, clinically approved carrier molecule called Captisol that markedly increased drug delivery to the brain.

"What's particularly exciting is that imatinib already is approved for use in humans, which suggests that we might be able to utilize this discovery to treat patients fairly soon," Gutstein said. He emphasized that the reformulated imatinib must first be tested for efficacy and safety in further animal studies, then in humans in a Phase I study.

Potential to reduce debilitating side effects

"Many patients in severe pain often refuse high doses of opioids because of the side effects, and they desperately need relief," Gutstein said. "We may be able to quickly translate this discovery and dramatically reduce the suffering endured by the sickest patients, and not just those with cancer."

Patients taking morphine and other opioids can experience side effects ranging from unpleasant to life-threatening in their intensity, including itching, constipation, nausea and breathing depression. Reducing morphine tolerance could allow the use of lower doses to relieve pain with fewer side effects.


'/>"/>

Contact: Scott Merville
smerville@mdanderson.org
713-792-0661
University of Texas M. D. Anderson Cancer Center
Source:Eurekalert

Related medicine news :

1. FemFlora Reformulated with New Complex of Probiotic Bacteria
2. Study reveals no impact of age on outcome in chronic myeloid leukemia patients treated with imatinib
3. Parkinsons disease: Excess of special protein identified as key to symptoms and possible new target for treatment with widely used anti-cancer drug imatinib
4. MU researchers develop tool that saves time, eliminates mistakes in diabetes care
5. New approach to thyroid surgery eliminates neck scar
6. Improved protocols for contrast agents eliminates new cases of nephrogenic systemic fibrosis
7. CT technique eliminates the need for X-rays in trauma patients with possible spinal fractures
8. MVP Health Care Eliminates Potential Health Insurance Coverage Gap for Many Young Adults
9. New Polycarbonate Sign Face Material Eliminates Hot Spots, Optimizes Light Uniformity in LED Back-Lit Signs
10. SBRT eliminates tumors with promising survival for early-stage inoperable lung cancer patients
11. A safer, more effective morphine may be possible with Indiana University discovery
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:6/26/2016)... Michigan (PRWEB) , ... June 26, 2016 , ... ... to fertility once they have been diagnosed with endometriosis. These women need a ... they also require a comprehensive approach that can help for preservation of fertility ...
(Date:6/25/2016)... Aliso Viejo, California (PRWEB) , ... June 25, 2016 , ... ... preset to fit their specific project," said Christina Austin - CEO of Pixel Film ... all fully customizable and all within Final Cut Pro X . Simply select ...
(Date:6/25/2016)... ... ... Friday, June 10, Van Mitchell, Secretary of the Maryland Department of Health and Mental ... exemplary accomplishments in worksite health promotion. , The Wellness at Work Awards took place ... BWI Marriott in Linthicum Heights. iHire was one of 42 businesses to receive an ...
(Date:6/24/2016)... ... ... June 19, 2016 is World Sickle Cell Observance Day. In an effort to ... treatments, Serenity Recovery Center of Marne, Michigan, has issued a pain management ... (SCD) is a disorder of the red blood cells, which can cause episodes of ...
(Date:6/24/2016)... ... June 24, 2016 , ... Dr. Amanda ... orthodontic treatment. Dr. Cheng has extensive experience with all areas of orthodontics, including ... accelerated osteogenic orthodontics. , Micro-osteoperforation is a revolutionary adjunct to orthodontic treatment. ...
Breaking Medicine News(10 mins):
(Date:6/26/2016)... -- Jazz Pharmaceuticals plc (Nasdaq: JAZZ ) ... Improvements Act of 1976, as amended ("HSR"), with respect ... Nasdaq: CPXX ) expired effective June 24, ... As previously announced on May 31, 2016, Jazz Pharmaceuticals ... which Jazz Pharmaceuticals has commenced a tender offer for ...
(Date:6/24/2016)... , June 24, 2016  Consumers have ... and regulators/payers have placed more emphasis on patient ... patient support programs in the pharmaceutical industry have ... medications. Consequently, pharmaceutical companies are focusing on becoming ... are providing products and services that improve health. ...
(Date:6/24/2016)... 2016   Bay Area Lyme Foundation , ... Center for Tick Borne Illness , Harvard Medical ... Hacking Medicine, University of California, Berkeley, and the ... five finalists of Lyme Innovation , the ... 100 scientists, clinicians, researchers, entrepreneurs, and investors from ...
Breaking Medicine Technology: