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Table 1 Drugs used to treat hematological and solid malignancies which are effective or highly effective in the inhibition of rRNA transcription or processing (modified from Burger et al., 2010) [5]

From: Treating hematological malignancies with drugs inhibiting ribosome biogenesis: when and why

 

inibition of rRNA synthesis

transcription

processing

Alkylating agents:

 Melphalan*

+

-

 Cisplatin*

+

-

 Oxaliplatin*

+

-

 Cyclophosphamide 1 *

+

-

Intercalating agents:

 Doxorubicin *

+

-

 Mitoxantrone *

+

-

 Actinomycin D *

+

-

 Mitomycin C

+

-

Antimetabolites:

 Methotrexate *

+

-

 5-Fluorouracil

-

+

 Topoisomerase inhibitors:

  

 Camptothecin

-

+

 Etoposide*

-

+

Kinase inhibitors:

 Flavopiridol*

-

+

 Roscovitine

-

+

 Rapamycin

+

-

Proteasome inhibitors:

 Bortezomib*

-

+

Translation inhibitors:

 Homoharringtonine*

-

+

Mitosis inhibitors:

 Vinblastine*

-

+

rRNA polymerase I inhibitors:

 CX-5461 2 *

+

-

  1. * drugs currently used or in clinical development for the treatment of lymphomas and leukemia
  2. 1 Cyclophosphamide is metabolized to acrolein, which is responsible for the inhibition of rRNA transcription [60, 61]
  3. 2 CX-5461 is in phase I clinical trial in patients with haematological malignancies and in phase I/II trial in patients with breast cancer