The primary metabolite of cyclophosphamide (CP, 1), i.e. 4-hydroxy-CP 2, has high pharmacological activity, but it is a very unstable compound. Chemical approaches to the stabilization involved in the substitution of the hydroxy group at the C 4-position, especially by a sulfoalkylthio-moiety. Withi
Inhibition of human B lymphocyte differentiation by a stable metabolite of cyclophosphamide (ASTA Z 7557, INN mafosfamide)
✍ Scribed by Andrzej Gorski; Grażyna Korczak-Kowalska
- Publisher
- Springer US
- Year
- 1984
- Tongue
- English
- Weight
- 194 KB
- Volume
- 2
- Category
- Article
- ISSN
- 0167-6997
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✦ Synopsis
We have evaluated the immunosuppressive effect of a new stable derivative of cyclophosphamide (ASTA Z 7557) on human lymphocyte immunoglobulin biosynthesis in vitro. When graded amounts of the drug are added to lymphocyte cultures stimulated with the helper T cell-dependent activator (PWM), a marked inhibition of B cell proliferation and differentiation occurs. Lymph node cells are particularly sensitive to the drug, while splenocytes are relatively resistant. The agent exerts only a minor effect on immunoglobulin synthesis triggered by a direct B cell stimulant (S. paratyphi bacteria).
📜 SIMILAR VOLUMES
ASTA Z 7557 is a stabilized cytostatic metabolite of cyclophosphamide which forms crystals at room temperature and releases 4-OH-cyclophosphamide in aqueous solution. The LD50/30 in mice after push injection is 417 mg/kg, after fractionated administration (q 6 hours X 4) 794 mg/kg. Daily treatment t
The precursor ASTA Z 7557 of the in vivo active metabolite 4-hydroxy-cyclophosphamide (4OH-Cy) of cyclophosphamide (Cy) was tested for selective effects on human T-lymphocytes' Fc gamma-receptor expression and certain immunoregulatory functions. It has been found that ASTA Z 7557 does not alter the