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Amsacrine


ACCESSION NB: DB00276 (APRD00064)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. [PubChem]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Antineoplastic Agents Intercalating Agents

ABSORPTION: Poorly absorbed

INDICATION:
For treatment of acute myeloid leukaemia.

PHARMACODYNAMICS:
Amsacrine is an aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects.

MECHANISM OF ACTION:
Amsacrine binds to DNA through intercalation and external binding. It has a base specificity for A-T pairs. Rapidly dividing cells are two to four times more sensitive to amsacrine than are resting cells. Amsacrine appears to cleave DNA by inducing double stranded breaks. Amsacrine also targets and inhibits topoisomerase II. Cytotoxicity is greatest during the S phase of the cell cycle when topoisomerase levels are at a maximum.

PROTEIN BINDING:
96-98%

METABOLISM:
Extensive, primarily hepatic, converted to glutathione conjugate.

TOXICITY:
Symptoms of overdose include nausea and vomiting, diarrhea, some cardiotoxicity (rarely).

AFECTED ORGANISMS:
Humans and other mammals