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Clinical pharmacokinetic study and sensitive effect of AK-2123
Purpose:
The pharmacokinetic parameters of a radiosensitizer, AK-2123 given to 10 lung cancer patients are represented and its sensitizing effect is evaluated.
Methods And Materials:
Ten patients with lung cancer: eight males, two females. The diagnosis was confirmed radiologically and pathologically. Seven patients were diagnosed with squamous cell cancer, two had adenocarcinoma, and one had nonsquamous cell lung cancer. AK-2123 was administered orally twice a week. The total dose per patient was 12.8-15.75 g. Radiotherapy was delivered 3 h after AK-2123 administration, 2 Gy per fraction. Blood samples were taken from the ear at 1, 3, 6, 9, 12, and 24 h after AK-2123 administration. The concentration of AK-2123 in plasma was measured by HPLC.
Results And Conclusions:
The Cm (maximum concentration of AK-2123 averaging from 10 patients) was 27.75 micrograms/mL, ranging 22.62-39.97 micrograms/mL, Tm (the time of getting Cm) 3 h. The data of the drug fitted a two-compartment open model. The mean parameteds of these cases were: rate constant K12 0.1658, K21 0.0671, Ke 0.0254, h-1; apparent volumes of distribution V1 18.6154, V2 51.2317, L; biological half life T1(2)a 1.0863, T1(2) alpha 2.7546, T1(2) beta 35.2064 h. The response to the treatment: CR four cases, PR four cases, NC two cases. So, AK-2123 may be a promising radiosensitizer.