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Human pharmacokinetics of 1-[2-[2-(4 pyridyl)-2-imidazolinyl-(1)]-ethyl]-3-(4-carboxyphenyl) urea (CGP 15720A)

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Summary

Pharmacokinetics of CGP 15720A have been studied in patients receiving this drug in a short I.V. infusion during its phase I clinical trial. Plasma decay was biphasic with a mean t1/2β of 4.9 ± 2.47h. The drug was cleared rapidly from plasma (7.02 ± 5.95 L/h). Renal clearance (4.13 ± 1.65 L/h) appears to be the major clearance pathway. The steady state volumes of distribution of the drug indicate limited tissue distribution for the drug. Studies with plasma and urine of patients receiving 14[C] GCP 15720A indicate that the drug is not metabolized. CGP 15720A could be measured in cerebrospinal fluid.

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References

  1. Creaven P, Madajewicz S, Pendyala L, Mittelman A, Takita H, Huben R, Cushman M: Phase I study of 1-(2-[2(4-pyridyl)-2-imidozoline-l-yl]-ethyl)-3-(4-carboxyphenyl)-urea (CGP 15720A) (Abstract). Proc Amer Soc Clin Oncol 4:49, 1985

    Google Scholar 

  2. Marxer A, Schmidt-Ruppin KH: Ureido-ethyl-imidazolines active against autochthonous diethyl nitrosamine induced epidermoid, papillary and adenocarcinomatous tumors of the respiratory tract of Syrian hamsters and against human bronchogenic carcinomas in nu/nu mice. Experientia 37:1123–1131, 1981

    Google Scholar 

  3. Brown MB, Engleman L, France JW, Hill MA, Jenrich RI, Toporce JD: BMDP Statistical Software, University of California. Los Angeles, 1981

    Google Scholar 

  4. Loo JK, Riegelman S: Assessment of pharmacokinetic constants from post infusion blood curves obtained after I.V. infusion. J Pharm Sci 59:53–55, 1970

    CAS  PubMed  Google Scholar 

  5. Gibaldi M, Perrier D: Pharmacokinetics. Marcel Dekker, New York, 1982

    Google Scholar 

  6. Rocci ML, Jusko WJ: Lagran program for area and moments in pharmacokinetic analysis. Computer Programs in Biomedicine 16:203, 1983

    Google Scholar 

  7. Kowarski CR, Kowarski AA: Simplified method for estimating volume of distribution at steady state. J Pharm Sci 69:1222, 1980

    Google Scholar 

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Pendyala, L., Madajewicz, S. & Creaven, P.J. Human pharmacokinetics of 1-[2-[2-(4 pyridyl)-2-imidazolinyl-(1)]-ethyl]-3-(4-carboxyphenyl) urea (CGP 15720A). Invest New Drugs 3, 375–381 (1985). https://doi.org/10.1007/BF00170761

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  • DOI: https://doi.org/10.1007/BF00170761

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