Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ)

Katherine Lu, Niramol Savaraj, Boh Seng Yap, Agop Y. Bedikian, Lynn G Feun, Robert S. Benjamin, Ti Li Loo

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

2,5′-Diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ) is an alkylating compound which has exhibited a broad spectrum of antitumor activity against a variety of experimental tumors, particularly those implanted intracranially. We have studied the clinical pharmacology of AZQ in 11 patients with various types of tumors. AZQ was administered at 1-12 mg/m2 daily for 5 days by i.v. infusion in 10-30 min. 14C-labelled AZQ was given on day 1 only. Blood and urine specimens were analyzed radiochemically and chromatographically. The plasma disappearance of unchanged AZQ was essentially biphasic, with an initial plasma t 1 2 of 1.4 ± 0.4 hr and a terminal t 1 2 of 45.5 ± 3.1 hr. The apparent volume of distribution was 14.2 ± 3.0 l/kg. The cumulative urinary excretion of unchanged AZQ was 4.3% in 24 hr and 8.6% in 96 hr. The total clearance of the drug was 200 ml/kg/hr. Cerebrospinal fluid AZQ concentration peaked 45-90 min after drug administration, reaching about 70% of that in plasma, and then declined at nearly the same rate.

Original languageEnglish
Pages (from-to)603-606
Number of pages4
JournalEuropean Journal of Cancer and Clinical Oncology
Volume19
Issue number5
DOIs
StatePublished - Jan 1 1983
Externally publishedYes

Fingerprint

diaziquone
Clinical Pharmacology
ethylenimine quinone
Pharmaceutical Preparations
Cerebrospinal Fluid
Neoplasms
Urine

ASJC Scopus subject areas

  • Oncology

Cite this

Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ). / Lu, Katherine; Savaraj, Niramol; Yap, Boh Seng; Bedikian, Agop Y.; Feun, Lynn G; Benjamin, Robert S.; Loo, Ti Li.

In: European Journal of Cancer and Clinical Oncology, Vol. 19, No. 5, 01.01.1983, p. 603-606.

Research output: Contribution to journalArticle

Lu, Katherine ; Savaraj, Niramol ; Yap, Boh Seng ; Bedikian, Agop Y. ; Feun, Lynn G ; Benjamin, Robert S. ; Loo, Ti Li. / Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ). In: European Journal of Cancer and Clinical Oncology. 1983 ; Vol. 19, No. 5. pp. 603-606.
@article{ceecf2e3525d4dd4a744e3ebb57be88b,
title = "Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ)",
abstract = "2,5′-Diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ) is an alkylating compound which has exhibited a broad spectrum of antitumor activity against a variety of experimental tumors, particularly those implanted intracranially. We have studied the clinical pharmacology of AZQ in 11 patients with various types of tumors. AZQ was administered at 1-12 mg/m2 daily for 5 days by i.v. infusion in 10-30 min. 14C-labelled AZQ was given on day 1 only. Blood and urine specimens were analyzed radiochemically and chromatographically. The plasma disappearance of unchanged AZQ was essentially biphasic, with an initial plasma t 1 2 of 1.4 ± 0.4 hr and a terminal t 1 2 of 45.5 ± 3.1 hr. The apparent volume of distribution was 14.2 ± 3.0 l/kg. The cumulative urinary excretion of unchanged AZQ was 4.3{\%} in 24 hr and 8.6{\%} in 96 hr. The total clearance of the drug was 200 ml/kg/hr. Cerebrospinal fluid AZQ concentration peaked 45-90 min after drug administration, reaching about 70{\%} of that in plasma, and then declined at nearly the same rate.",
author = "Katherine Lu and Niramol Savaraj and Yap, {Boh Seng} and Bedikian, {Agop Y.} and Feun, {Lynn G} and Benjamin, {Robert S.} and Loo, {Ti Li}",
year = "1983",
month = "1",
day = "1",
doi = "10.1016/0277-5379(83)90175-X",
language = "English",
volume = "19",
pages = "603--606",
journal = "European Journal of Cancer and Clinical Oncology",
issn = "0277-5379",
publisher = "Pergamon Press",
number = "5",

}

TY - JOUR

T1 - Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ)

AU - Lu, Katherine

AU - Savaraj, Niramol

AU - Yap, Boh Seng

AU - Bedikian, Agop Y.

AU - Feun, Lynn G

AU - Benjamin, Robert S.

AU - Loo, Ti Li

PY - 1983/1/1

Y1 - 1983/1/1

N2 - 2,5′-Diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ) is an alkylating compound which has exhibited a broad spectrum of antitumor activity against a variety of experimental tumors, particularly those implanted intracranially. We have studied the clinical pharmacology of AZQ in 11 patients with various types of tumors. AZQ was administered at 1-12 mg/m2 daily for 5 days by i.v. infusion in 10-30 min. 14C-labelled AZQ was given on day 1 only. Blood and urine specimens were analyzed radiochemically and chromatographically. The plasma disappearance of unchanged AZQ was essentially biphasic, with an initial plasma t 1 2 of 1.4 ± 0.4 hr and a terminal t 1 2 of 45.5 ± 3.1 hr. The apparent volume of distribution was 14.2 ± 3.0 l/kg. The cumulative urinary excretion of unchanged AZQ was 4.3% in 24 hr and 8.6% in 96 hr. The total clearance of the drug was 200 ml/kg/hr. Cerebrospinal fluid AZQ concentration peaked 45-90 min after drug administration, reaching about 70% of that in plasma, and then declined at nearly the same rate.

AB - 2,5′-Diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ) is an alkylating compound which has exhibited a broad spectrum of antitumor activity against a variety of experimental tumors, particularly those implanted intracranially. We have studied the clinical pharmacology of AZQ in 11 patients with various types of tumors. AZQ was administered at 1-12 mg/m2 daily for 5 days by i.v. infusion in 10-30 min. 14C-labelled AZQ was given on day 1 only. Blood and urine specimens were analyzed radiochemically and chromatographically. The plasma disappearance of unchanged AZQ was essentially biphasic, with an initial plasma t 1 2 of 1.4 ± 0.4 hr and a terminal t 1 2 of 45.5 ± 3.1 hr. The apparent volume of distribution was 14.2 ± 3.0 l/kg. The cumulative urinary excretion of unchanged AZQ was 4.3% in 24 hr and 8.6% in 96 hr. The total clearance of the drug was 200 ml/kg/hr. Cerebrospinal fluid AZQ concentration peaked 45-90 min after drug administration, reaching about 70% of that in plasma, and then declined at nearly the same rate.

UR - http://www.scopus.com/inward/record.url?scp=0020549191&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0020549191&partnerID=8YFLogxK

U2 - 10.1016/0277-5379(83)90175-X

DO - 10.1016/0277-5379(83)90175-X

M3 - Article

C2 - 6683631

AN - SCOPUS:0020549191

VL - 19

SP - 603

EP - 606

JO - European Journal of Cancer and Clinical Oncology

JF - European Journal of Cancer and Clinical Oncology

SN - 0277-5379

IS - 5

ER -