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首頁產業資訊製藥報導製藥產業「2017 未來科技展」技術專題報導─可預防化學誘導腸道損傷與大腸癌之創新藥物

「2017 未來科技展」技術專題報導─可預防化學誘導腸道損傷與大腸癌之創新藥物

來源 : 未來科技展
update : 2018/01/04
技術名稱: 可預防化學誘導腸道損傷與大腸癌之創新藥物
An novel drug for preventing chemical-induced intestinal damage and colorectal cancer
 
計畫單位: 高雄醫學大學
Kaohsiung medical university
 
技術說明: 葡萄醣醛酸化(glucuronidation)是肝臟解毒的主要路徑,化療藥或有毒物質會經由此葡萄醣醛酸化代謝而降低毒性並排出體外,但是當葡萄醣醛酸化的代謝物進入腸道後,會被腸道菌所表現的eβG再度回復成有毒物質,因而造成腸道受損與腹瀉,久而久之更可能導致腸道病變跟大腸癌。然而,目前臨床上多是利用止瀉劑來舒緩腹瀉症狀,但無法避免腸道被破壞,而且現今更是缺乏可以預防大腸癌生成的藥物被開發。為了解決這個臨床仍未滿足的需求,我們開發了腸道菌eβG專一性抑制劑,作為”預防化學誘導腸道損傷與大腸癌之創新藥物”。
 
此腸道菌eβG專一性抑制劑,可作為:

 (一)化療藥口服佐劑,與化療藥合併使用,防止化療藥誘發的腸道損傷及腹瀉,以改善病人生活品質,並且增加病人對藥物的耐受性而增加療效;

(二)預防大腸癌創新藥物,透過防止解毒後的致癌劑再度回復毒性,來避免化學誘發腸道病變及腫瘤生成。

目前此腸道菌eβG專一性抑制劑作為預防化療副作用與大腸癌,已經申請PCT專利合作條約、美國專利臨時案與台灣(中華民國)專利。
 
Glucuronidation is a major pathway for detoxification in the liver. Drugs and toxic chemicals are conjugated with glucuronide acid to be inactive form through this pathway. However, when glucuronide conjugates enter the intestine, they are reactivated by E. coli expressing G (eG) back to toxic form, thus damaging the intestine and inducing diarrhea, which is likely to cause carcinogenesis and colorectal cancer. The current treatment is using antidiarrheal agent to release the diarrhea symptom but the damage still persist. In addition, there are no clinical drug been developed to prevent colon cancer. In order to meet the unmet clinical need, we have successfully developed eβG specific inhibitor as a novel drug for preventing chemical-induced damage and colon cancer. The inhibitor can be developed as:
 1. Chemotherapy adjuvant, be combined with chemo drug to prevent chemotherapy -induced intestinal damage and diarrhea, thus improving patients’ quality of life and increasing patient’s drug tolerance to increase therapy efficacy.
 2. Chemoprevention drug, to prevent reactivating of the carcinogen in the intestine and thus reducing chemo-induced carcinogenesis and colon cancer.
 We have applied the novel inhibitor and its derivatives and their function for patent protection, including PCT, provisional application for patent in the US, and the Taiwan (ROC) patent.