Clinical pharmacokinetic study and sensitive effect of AK-2123.
OBJECTIVE
The pharmacokinetic parameters of a radiosensitizer, AK-2123 given to 10 lung cancer patients are represented and its sensitizing effect is evaluated.


METHODS
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.


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.
Huan
L C
LC
Institute of Radiation Medicine Beijing, China.
Hua
B Y
BY
D000328:Adult; D000368:Aged; D005260:Female; D006801:Humans; D008175:Lung Neoplasms / Q000378:metabolism / Q000532:radiotherapy; D008297:Male; D008875:Middle Aged; D011838:Radiation-Sensitizing Agents / Q000493:pharmacokinetics*; D014230:Triazoles / Q000493:pharmacokinetics* / Q000494:pharmacology
D011838:Radiation-Sensitizing Agents; D014230:Triazoles; C072690:AK 2123