Clinical pharmacokinetic study and sensitive effect of AK-2123
- Institute of Radiation Medicine, Beijing (China)
- North TaiPing Road Hospital, Beijing (China)
The pharmacokinetic parameters of a radiosensitizer, AK-2123 (a nitrotriazole deriv.) given to 10 lung cancer patients are represented and its sensitizing effect is evaluated. 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. The C[sub m] (maximum concentration of AK-2123 averaging from 10 patients) was 27.75 [mu]g/mL, ranging 22.62-39.97 [mu]g/mL, T[sub m] (the time of getting C[sub m]) 3 h. The data of the drug fitted a two-compartment open model. The mean parameters of these cases were: rate constant K12 0.1658, K21 0.0671, Ke 0.0254, h[sup [minus]1]; apparent volumes of distribution V[sub 1] 18.6154, V[sub 2] 51.2317, L; biological half life T[sub 1]2a 1.0863, T[sub 1]2[alpha] 2.7546, T[sub 1]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. 5 refs., 4 figs., 2 tabs.
- OSTI ID:
- 6869572
- Journal Information:
- International Journal of Radiation Oncology, Biology and Physics; (United States), Vol. 29:3; ISSN 0360-3016
- Country of Publication:
- United States
- Language:
- English
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