Etoposide: A Semisynthetic Epipodophyllotoxin Chemistry, Pharmacology, Pharmacokinetics, Adverse Effects and Use as an Antineoplastic Agent

@article{Sinkule1984EtoposideAS,
  title={Etoposide: A Semisynthetic Epipodophyllotoxin Chemistry, Pharmacology, Pharmacokinetics, Adverse Effects and Use as an Antineoplastic Agent},
  author={Joseph A. Sinkule},
  journal={Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy},
  year={1984},
  volume={4}
}
  • J. Sinkule
  • Published 4 March 1984
  • Medicine
  • Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
Etoposide (VP 16) is a semi‐synthetic derivative of 4'‐demethylepipodophyllotoxin, a naturally occurring compound synthesized by the North American May apple (Podophyllum peltatum) and the Indian species Podophyllum emodi Wallich. Although podophyllotoxins are classical spindle poisons causing inhibition of mitosis by blocking mitrotubular assembly, etoposide inhibits cell cycle progression at a premitotic phase (late S and G2), probably via inhibition of DNA synthesis. There appears to be a… Expand
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4'-Demethyl-epipodophyllotoxin thenylidene glucoside (VM 26), a podophyllum compound with a new mechanism of action.
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The new podophyllotoxin glucoside derivative VM 26 was found to have a high cytostatic activity in cell cultures and inhibits entry of cells into mitosis or destroys cells preparing for mitosis, one of its biochemical effects is inhibition of thymidine uptake. Expand
The epipodophyllotoxin derivatives VM-26 and VP-16-213, 1976-1979, a review.
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It seems possible at present to justify a discontinuation of VM-26 in order to concentrate the efforts on VP 16-213, which is among the most active drugs in small-cell carcinoma of the lung. Expand
A clinical trial of the oral form of 4′‐demethyl‐epipodophyllotoxin‐β‐D ethylidene glucoside (NSC 141540) VP 16–213
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A clinical trial of the oral form of VP 16‐213 (NSC‐141540), a semisynthetic podophyllotoxin, was undertaken, with partial remissions (PR) and improvement (IMP) seen. Expand
Schedule dependency of the antileukemic activity of the podophyllotoxin-derivative VP 16-213 (NSC-141540) in L1210 leukemia.
TLDR
Divided treatment every 3 hours for 24 hours demonstrated a significant superiority over a single treatment, which together with the mechanism of action could indicate, that VP 16–213 is a cell cycle specific drug. Expand
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TLDR
VP-16-213 (etoposide) is an orally and parenterally active antineoplastic agent synthesized from podophyllum extracts of a common North American plant, the May apple or mandrake, which is active in a variety of animal tumors and leukemias. Expand
Combination chemotherapy with 4'Demethylepipodophyllotoxin 9-(4,6-0-ethylidene-beta-D-glucopyranoside), VP 16-213 (NSC 141540) in L1210 leukemia.
TLDR
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Delayed toxicity of epipodophyllotoxin derivatives (VM 26 and VP 16-213), due to a local effect.
TLDR
The experimental results support the recommendation not to use these drugs in man by the intraperitoneal or intrapleural route or to inject them into the cerebrospinal fluid, and do not support the contention that in clinical practice such a delayed toxicity may occur when the usual routes of administration are employed. Expand
Activity of a new glycosidic lignan derivative (VP 16-213) related to podophyllotoxin in experimental tumors
Abstract -VP 16-213 (4′-demethyl-epipodophylloloxin ethylidene-β-D-glucoside) is closely related to VM 26 in chemical structure and biological activity: it inhibits entry of cells into mitosis asExpand
[Initial results with a epipodophyllotoxin derivative VP 16-213 in the treatment of acute leukemia].
TLDR
Ten acute leukemia patients were treated with the new cytostatic agent VP 16-213, and one complete and two partial remissions were achieved, while one patient showed brief clinical improvement. Expand
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