Key binding of Abiraterone (Zytiga) with the enzyme CYP17
Structure of Abiraterone (Zytiga)
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Reduction of PSA and Tumour Volume by Zytiga
Saturday, 29 September 2012
Akt Inhibitor Zytiga Combo
Clinical trials are underway on the combination of the Akt inhibitor GDC-0068 in combination with Zytiga and Prednisone. Akt is a downstream target of PI3 Kinase signalling involved in drug resistance and tumour progression. GDC-0068 is an inhibitor of Akt with an IC50 of 5 nM and a 400 mg dose has a half life of 24 hours. Chemotherapy can induce Akt activation in resistant cells and so an Akt inhibitor can overcome resistance to chemotherapy. PI3 Kinase / Akt signalling is involved in Zytiga resistance and so an inhibitor such as GDC-0068 may overcome Zytiga resistance. GDC-0068 is being developed by Genentech Roche and is a selective and potent inhibitor of Akt also known as PKB. Zytiga in combination with Prednisone is now the Standard Of Care in prostate cancer therapy and so many agents are being trialled in combination with these agents. The Zytiga GDC-0068 combo offers a rational approach to overcoming Zytiga resistance and prolonging its duration of action.
Key binding of Abiraterone (Zytiga) with the enzyme CYP17
Structure of Prednisone (needed to overcome potassium deficiency Hypokalemia side effect of Zytiga)
Structure of Abiraterone (Zytiga)
Reduction of PSA and Tumour Volume by Zytiga
Key binding of Abiraterone (Zytiga) with the enzyme CYP17
Structure of Abiraterone (Zytiga)
Reduction of PSA and Tumour Volume by Zytiga
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