II. Indications

  1. FDA Approved (often combined with other agents)
    1. Ovarian Cancer
    2. Cervical Cancer
  2. Off-Label
    1. Acute Myelogenous Leukemia (AML)
    2. CNS Malignancy (including CNS Lymphoma)
    3. Ewing Sarcoma
    4. Neuroblastoma
    5. Ovarian Cancer (metastatic)
    6. Rhabdomyosarcoma

III. Mechanism

  1. See Mitotic Inhibitor Chemotherapy
  2. Irinotecan is a semisynthetic derivative of camptothecin with antineoplastic activity
    1. Camptothecin extracted from the Asian tree Camptotheca acuminata ("Happy Tree")
    2. Camptothecin is a cytotoxic quinoline-based alkaloid
  3. Topotecan is active without metabolism
    1. Contrast with Irinotecan, a similar drug, but that requires metabolism to SN-38 for activity
    2. Topotecan is considered less potent than SN-38, the active metabolite of Irinotecan
  4. Topotecan is a Topoisomerase Inhibitor
    1. Binds to topoisomerase 1, inhibiting DNA ligation
    2. DNA breaks accumulate
    3. Inhibits DNA Replication and transcription
    4. Arrests Cell Cycle in S phase
    5. Results in cell apoptosis and death

IV. Medications

  1. Oral Capsules: 0.25 mg and 1 mg
  2. Powder for IV Injection Solution: 4 mg

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Myelosuppression (Bone Marrow suppression)
    1. Neutropenia
  2. Bleeding (may be severe)
  3. Interstitial Lung Disease

VII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception (including one month after Chemotherapy completed)
  3. Monitoring
    1. Complete Blood Count

IX. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Ontology: Topotecan (C0146224)

Definition (NCI_NCI-GLOSS) A drug used to treat certain types of ovarian cancer, lung cancer, and cervical cancer. Topotecan is a type of topoisomerase inhibitor.
Definition (NCI) A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Topotecan inhibits topoisomerase I activity by stabilizing the topoisomerase I-DNA covalent complexes during S phase of cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery.
Definition (CSP) antineoplastic drug which acts as a DNA topoisomerase inhibitor.
Definition (MSH) An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D019772
SnomedCT 108779005, 372536007
LNC LP172582-1, MTHU046380
English 9 Dimethylaminomethyl 10 hydroxycamptothecin, 9-Dimethylaminomethyl-10-hydroxycamptothecin, Hycamtamine, (s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]-quinoline-3,14(4H,12H)-dione, 9-[(dimethylamino)methyl]-10-hydroxy-(20S)-camptothecin, Topotecan Lactone, Topotecan [Chemical/Ingredient], topotecan, TOPOTECAN, Topotecan (product), Topotecan (substance), hycamptamine, TOPO, Topotecan, Hycamptamine
Swedish Topotecan
Czech topotekan
Finnish Topotekaani
Russian TOPOTEKAN, ТОПОТЕКАН
Japanese ハイカムチン注射用, ハイカムチン, ノギテカン, 塩酸ノギテカン, トポテカン, 塩酸トポテカン, ノギテカン塩酸塩, トポテカン塩酸塩
Spanish topotecano (producto), topotecano, topotecán (producto), topotecano (sustancia), topotecán (sustancia), topotecán, Topotecan
French 9-diméthylaminométhyl-10-hydroxycamptothécine, Hycamtamine, 9-(diméthylamino)méthyl-10-hydroxycamptothécine, Topotécane
Polish Topotekan
German Topotecan
Italian Topotecan
Portuguese Topotecan