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Nitrosoureas, triazenes, alkyl sulfonates, aziridines and related alkylatorsUsed in a few countriesSyntheticNeeds review

Ranimustine

Also known as MCNU, methyl 6-[3-(2-chloroethyl)-3-nitrosoureido]-6-deoxy-alpha-D-glucopyranoside

A water-soluble chloroethyl nitrosourea linked to a sugar, known as MCNU. Reports from 1979 to 1990 test it in mouse tumours and mainly in chronic myeloid leukaemia and other myeloproliferative disorders.

From discovery to approval

  1. 1978 · Earliest report found

    A 1978 review of Japanese drug development lists MCNU, with GANU, as ready for phase I study in Japan. A 1979 report describes MCNU as a new water-soluble nitrosourea active against several mouse tumours, and phase I and II reports followed in 1983. Its synthesis and developers were not traced.[2][3][4][5][6]

  2. No approval is recorded on this site.

How it works

Its chemical name shows a 2-chloroethyl nitrosourea. A 2017 review of the chloroethylating nitrosoureas (which does not name ranimustine) says drugs of this type alkylate DNA bases and form interstrand crosslinks. No ranimustine-specific mechanism study was read.[1]

Where it came from and why

The sources read do not say why it was made. A 1988 report calls it a new water-soluble nitrosourea derivative and tested it against busulfan in chronic myeloid leukaemia.

Cancers

  • Chronic myeloid leukaemia

    A randomised comparison with busulfan in chronic-phase CML enrolled 40 patients on MCNU and 37 on busulfan.[6]

  • Polycythaemia vera and thrombocythaemia

    A 1990 Japanese-journal review (English abstract) reports very good responses in chronic myeloid leukaemia, polycythaemia vera and thrombocythaemia and moderate responses in lymphoma or myeloma.[7]

Worth knowing

  • In the randomised comparison with busulfan in chronic-phase CML, the median time to complete remission was 50 days with MCNU (40 patients) and 126 days with busulfan (37 patients; p < 0.05), with no difference in complete remission rate, mortality, blast crisis or survival.[6]
  • A 1990 review abstract reports a complete remission rate of 82% in CML, maintained for 2 to 18 months after a single administration.[7]

References

  1. Nikolova T, Roos WP, Krämer OH, Strik HM, Kaina B. Chloroethylating nitrosoureas in cancer therapy: DNA damage, repair and cell death signaling. Biochim Biophys Acta Rev Cancer. 2017;1868(1):29-39. PubMedDOI
  2. Sakurai Y. Synthetic analogs of antitumor drugs under development in Japan. Recent Results Cancer Res. 1978;63:272-81. PubMedDOI
  3. Sekido S, Ninomiya K, Iwasaki M. Biologic activity of MCNU: a new antitumor agent. Cancer Treat Rep. 1979;63(6):961-70. PubMed
  4. Kanamaru A, Nagai K, Fujita S, Masaoka T, Takubo T, Kitani T, et al. [Phase I study on oral administration of methyl-6-[[[(2-chloroethyl) nitrosoamino] carbonyl] amino]-6-deoxy-alpha-D-glucopyranoside (MCNU)]. Gan To Kagaku Ryoho. 1983;10(8):1831-7. PubMed
  5. Masaoka T, Kimura K, Miyazaki T, Sakurada K, Saitoh H, Morioka M, et al. [Phase II study with methyl-6[[[2-chloroethyl) nitrosoamino] carbonyl] amino]-6-deoxy-alpha-D-glucopyranoside (MCNU) in hematological malignancies]. Gan To Kagaku Ryoho. 1983;10(6):1518-23. PubMed
  6. Hiraoka A, Masaoka T, Shibata H, Miyazaki T, Nakamura T, Yasunaga K, et al. A new nitrosourea derivative for the treatment of chronic myelogenous leukemia. Leuk Res. 1988;12(6):487-90. PubMedDOI
  7. Masaoka T. [Ranimustine]. Gan To Kagaku Ryoho. 1990;17(2):301-7. PubMed