Oral melphalan kinetics

David S Alberts, Sai Y. Chang, H. S. George Chen, Thomas L. Evans, Thomas E. Moon

Research output: Contribution to journalArticle

85 Citations (Scopus)

Abstract

The systemic availability of melphalan after oral administration is not well known. Most patients are put on a fixed oral dosage regimen. We have studied the disposition of melphalan in 14 patients after single oral doses. Five were also studied after receiving the same dose intravenously. Oral melphalan had a mean plasma terminal phase half-life (t 1 2) of 90+- 17 min. The mean area under the plasma concentration: time curve (CXT) was 53 ± 33 μg · min/ml Urinary excretion of oral melphalan averaged 10.9 ± 4.9% during the first 24 hr. The CXT ratio (oral: intravenous) for the 5 patients studied after both oral and intravenous melphalan (0.6 mg/kg) ranged between 0.25 and 0.89 and averaged 0.56. After oral dosing in 14 fasting patients, the time at which melphalan first appeared in the plasma varied between 15 min and 6 hr. In a myeloma patient who took oral melphalan, no melphalan was found in plasma or urine up to 24 hr. Some instances of failure of tumor response to oral melphalan may be due to inadequate bioavailability rather than inherent tumor resistance.

Original languageEnglish (US)
Pages (from-to)737-745
Number of pages9
JournalClinical Pharmacology and Therapeutics
Volume26
Issue number6
StatePublished - Dec 1979

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Melphalan
Biological Availability
Oral Administration
Half-Life
Fasting
Neoplasms
Urine

ASJC Scopus subject areas

  • Pharmacology

Cite this

Alberts, D. S., Chang, S. Y., George Chen, H. S., Evans, T. L., & Moon, T. E. (1979). Oral melphalan kinetics. Clinical Pharmacology and Therapeutics, 26(6), 737-745.

Oral melphalan kinetics. / Alberts, David S; Chang, Sai Y.; George Chen, H. S.; Evans, Thomas L.; Moon, Thomas E.

In: Clinical Pharmacology and Therapeutics, Vol. 26, No. 6, 12.1979, p. 737-745.

Research output: Contribution to journalArticle

Alberts, DS, Chang, SY, George Chen, HS, Evans, TL & Moon, TE 1979, 'Oral melphalan kinetics', Clinical Pharmacology and Therapeutics, vol. 26, no. 6, pp. 737-745.
Alberts DS, Chang SY, George Chen HS, Evans TL, Moon TE. Oral melphalan kinetics. Clinical Pharmacology and Therapeutics. 1979 Dec;26(6):737-745.
Alberts, David S ; Chang, Sai Y. ; George Chen, H. S. ; Evans, Thomas L. ; Moon, Thomas E. / Oral melphalan kinetics. In: Clinical Pharmacology and Therapeutics. 1979 ; Vol. 26, No. 6. pp. 737-745.
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