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Innovation
Highly Selective c-Src Tyrosine Kinase Inhibitors
University of Michigan
posted on 01/25/2012
Highly Selective c-Src Tyrosine Kinase Inhibitors
Innovation Details
Detailed Description
UM File # 5120
Background
Worldwide approximately 22 million people are living with cancer and nearly 7 million people die each year. Despite the availability of improved drugs, cancer is still the second cause of death in industrialized countries. By 2020, cancer incidence is expected to increase to 14 million each year, compared to 10 million in 2010. In 2010, worldwide cancer treatment market revenues were ~$60 billion, and they are expected to reach ~$80 billion in 2013. Currently there are two major categories for oncology drugs: traditional cytotoxic chemotherapies, and molecularly targeted drugs that specifically modulate the activity of one of more proteins involved in cancer. Molecularly targeted therapies entered the market about ten years ago and have enjoyed very high success rates – in fact, the majority of sales growth is attributed to an increasing approval of targeted cancer therapies. In general, targeted therapies have a much higher therapeutic index compared to traditional therapies, and have significantly lower side-effects. This leads to better drug tolerability, better patient compliance, and improved quality of life for the patient. However, even targeted therapies exhibit unwanted side-effects, and therefore strategies to minimize toxicity are necessary.
Technology Description
Researchers at the University of Michigan have developed a highly selective inhibitor of non-receptor tyrosine kinase c-Src which is significantly less toxic in cellular models of cancer. The only currently FDA-approved c-Src inhibitor dasatinib has been found to inhibit more than 40 different kinases with high affinity, leading to toxic side-effects of this drug. Researchers tested their newly developed inhibitor against c-Src and a panel of homologous kinases, and found that it showed exquisite selectivity for c-Src. This compound has similar potency to dasatinib in cellular models of cancer, but it is significantly less toxic.
Applications
• New compound that is a selective inhibitor of c-Src tyrosine kinase
• New therapy for c-Src-dependent cancers with lower toxicity
Advantages
• No c-Src selective inhibitor on the market
• Selective inhibitor of c-Src can improve toxicity profile over current therapies
• Cost-savings through shortened time-lines
• Decreased toxicity can shorten development / FDA approval time
Background
Worldwide approximately 22 million people are living with cancer and nearly 7 million people die each year. Despite the availability of improved drugs, cancer is still the second cause of death in industrialized countries. By 2020, cancer incidence is expected to increase to 14 million each year, compared to 10 million in 2010. In 2010, worldwide cancer treatment market revenues were ~$60 billion, and they are expected to reach ~$80 billion in 2013. Currently there are two major categories for oncology drugs: traditional cytotoxic chemotherapies, and molecularly targeted drugs that specifically modulate the activity of one of more proteins involved in cancer. Molecularly targeted therapies entered the market about ten years ago and have enjoyed very high success rates – in fact, the majority of sales growth is attributed to an increasing approval of targeted cancer therapies. In general, targeted therapies have a much higher therapeutic index compared to traditional therapies, and have significantly lower side-effects. This leads to better drug tolerability, better patient compliance, and improved quality of life for the patient. However, even targeted therapies exhibit unwanted side-effects, and therefore strategies to minimize toxicity are necessary.
Technology Description
Researchers at the University of Michigan have developed a highly selective inhibitor of non-receptor tyrosine kinase c-Src which is significantly less toxic in cellular models of cancer. The only currently FDA-approved c-Src inhibitor dasatinib has been found to inhibit more than 40 different kinases with high affinity, leading to toxic side-effects of this drug. Researchers tested their newly developed inhibitor against c-Src and a panel of homologous kinases, and found that it showed exquisite selectivity for c-Src. This compound has similar potency to dasatinib in cellular models of cancer, but it is significantly less toxic.
Applications
• New compound that is a selective inhibitor of c-Src tyrosine kinase
• New therapy for c-Src-dependent cancers with lower toxicity
Advantages
• No c-Src selective inhibitor on the market
• Selective inhibitor of c-Src can improve toxicity profile over current therapies
• Cost-savings through shortened time-lines
• Decreased toxicity can shorten development / FDA approval time
File Number: 5120
IP Protection
| Patent Number(s): | 61/527768 |
|---|
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