Influence of oral BM 12531 (INN azimexon) on immune response in untreated cancer patients

Heim, Manfred; Massner, B.; Knebel, L.; Stosiek, U; Boerner, D; Bicker, U.

doi:10.1007/bf00200317

Cited by 5 publications

(4 citation statements)

References 5 publications

(10 reference statements)

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“…These symptoms were accompanied by enlargement of the spleen. Clinical investigations revealed after very high doses also hemolysis, which is probably toxic (Heim et al 1981) and arises from changes in the hemoglobin molecule.…”

Section: Discussionmentioning

confidence: 98%

The action of azimexone on the cells of the hemopoietic system in mice, especially after damage with X-rays

Friedberg

Mengel

Schlick

1983

Radiat Environ Biophys

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Mice were exposed to single doses of whole body X-irradiation (1 - 2 - 4 Gy) or were treated with sulphur mustard (15 mg/kg body weight i.p.). This treatment caused a reduction of the pluripotent stem cells in the bone marrow, of the total count of nucleated bone marrow cells in the femora and of the WBC in the peripheral blood. The size distribution of the bone marrow cells showed three separate peaks. From the histological examination of the bone marrow of X-irradiated mice it was deduced that the first peak represents erythrocytes, the second lymphocytes and the third peak the precursors of red and white blood cells. Multiple doses (25 - 50 - 100 mg/kg body weight) of azimexone, an immunomodulating substance, led after moderate doses of X-rays (2 Gy) or sulphur mustard to a more rapid recovery of the various parameters. In particular a stimulant action of azimexone on the pluripotent stem cells of mice not subjected to the injurious agents could also be demonstrated.

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Section: Discussionmentioning

confidence: 98%

The action of azimexone on the cells of the hemopoietic system in mice, especially after damage with X-rays

Friedberg

Mengel

Schlick

1983

Radiat Environ Biophys

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“…Azimexon (4) was tested in 30 cancer patients in a double blind study at a dose of 300 mg orally for 7 days [15]. As expected, there was a significant rise in the percentage of activated T lymphocytes [16].…”

Section: Clinical Studies On Azimexon and Ciamexonmentioning

confidence: 99%

Chemistry and Pharmacology of Imexon and Related Cyanoaziridines

Wa¹,

Rt²

2012

CMC

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Following the demonstration that addition of a 2-cyano group to aziridines prevented DNA alkylation and thus reduced toxicity, many novel 2-cyanoaziridines were synthesized and evaluated as immunomodulating and antitumor agents. They typically reacted with thiols such as cysteine, depleting them and allowing the accumulation of reactive oxygen species. Two of these compounds, azimexon and ciamexon, showed activity against tumors in clinical trials. Imexon was produced by cyclization of 2-cyanoaziridine-1- carboxamide in the presence of hydroxide ions. The two enantiomers were prepared by a process involving chiral chromatography. They were equipotent against cultured tumor cells. Imexon also reacts with thiols and it is especially potent against multiple myeloma in cell cultures. An efficient chemical synthesis and a lyophilization formulation of imexon as a water soluble, injectible drug, were developed. In Phase I and I/II clinical trials imexon showed hints of activity against a variety of tumors, but a randomized double-blind Phase II trial of imexon plus gemcitabine versus gemcitabine alone in pancreatic cancer showed no enhancement of activity above that of gemcitabine alone. This result was disappointing because in cell culture and mice the two compounds were synergistic. Based on a complete response in a Phase I trial, a new Phase II clinical trial of imexon is underway in non-Hodgkins lymphoma.

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“…However, the frequent reports of toxic responses to bacterial vaccines, together with difficulties in standardizing preparations [56] is leading to a greater interest in more well defined agents including interferons [4,5] and synthetic compounds such as azimexon [42]. However, the frequent reports of toxic responses to bacterial vaccines, together with difficulties in standardizing preparations [56] is leading to a greater interest in more well defined agents including interferons [4,5] and synthetic compounds such as azimexon [42].…”

Section: Clinical Trialsmentioning

confidence: 99%

Manipulation of host resistance in cancer therapy

Baldwin

1982

Springer Semin Immunopathol

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Influence of oral BM 12531 (INN azimexon) on immune response in untreated cancer patients

Abstract: Summary. To evaluate the immune-stimulating properties of 2-(2-cyanaziridinyl-

Cited by 5 publications

References 5 publications

The action of azimexone on the cells of the hemopoietic system in mice, especially after damage with X-rays

The action of azimexone on the cells of the hemopoietic system in mice, especially after damage with X-rays

Chemistry and Pharmacology of Imexon and Related Cyanoaziridines

Manipulation of host resistance in cancer therapy

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