Topotecan
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Manufacturer Warnings
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FDA Labeling Changes
There are currently no FDA labeling changes available for this drug.
Uses
Topotecan Injection is indicated for the treatment of:
- small cell lung cancer sensitive disease after failure of first-line chemotherapy. In clinical studies submitted to support approval, sensitive disease was defined as disease responding to chemotherapy but subsequently progressing at least 60 days (in the Phase 3 study) or at least 90 days (in the Phase 2 studies) after chemotherapy [see Clinical Studies (14)].
Topotecan Injection in combination with cisplatin is indicated for the treatment of:
- stage IV-B, recurrent, or persistent carcinoma of the cervix which is not amenable to curative treatment with surgery and/or radiation therapy.
History
There is currently no drug history available for this drug.
Other Information
Topotecan is a semi-synthetic derivative of camptothecin and is an anti-tumor drug with topoisomerase I-inhibitory activity.
The chemical name for topotecan free base is (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. It has the molecular formula C23H23N3O5 and a molecular weight of 421.45.
Topotecan has three pKa values: pKa1 = 10.50 corresponding to the benzyldimethylamino group, pKa2 = 6.99 corresponding to the phenol group and pKa3 = 0.60 corresponding to the quinoline group.
As formulated in Topotecan Injection, topotecan has the following structural formula:
where n is >1, corresponding to HCl added to adjust the pH to approximately 2.0 to 2.5.
Topotecan Injection is supplied as a sterile, non-pyrogenic, clear, yellow solution at a topotecan free base concentration of 4 mg/4 mL (1 mg/mL), 3 mg/3 mL (1 mg/mL), and 1 mg/mL available in multiple dose vials. Each mL of Topotecan Injection contains topotecan hydrochloride equivalent to 1 mg of topotecan as free base, 5 mg tartaric acid, NF, and water for injection, USP. Hydrochloric acid and/or sodium hydroxide may be used to adjust the pH.. The hydrochloride salt of topotecan is soluble in water and melts with decomposition at 213°C to 218°C.
The solution must be diluted before administration by intravenous infusion.
Sources
Topotecan Manufacturers
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Sandoz Inc
![Topotecan Injection [Sandoz Inc]](/wp-content/themes/bootstrap/assets/img/loading2.gif)
Topotecan | Sandoz Inc
Prior to administration of the first course of Topotecan Injection, patients must have a baseline neutrophil count of >1,500 cells/mm3 and a platelet count of >100,000 cells/mm3.
2.1 Small Cell Lung CancerRecommended Dosage
The recommended dose of topotecan is 1.5 mg/m2 by intravenous infusion over 30 minutes daily for 5 consecutive days, starting on day 1 of a 21-day course. In the absence of tumor progression, a minimum of 4 courses is recommended because tumor response may be delayed. The median time to response in 4 small cell lung cancer trials was 5 to 7 weeks.Dosage Modification Guidelines
In the event of severe neutropenia (defined as <500 cells/mm3) during any course, reduce the dose by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. Alternatively, in the event of severe neutropenia, administer G-CSF (granulocyte-colony stimulating factor) following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hours after completion of topotecan administration). In the event the platelet count falls below 25,000 cells/mm3, reduce doses by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. 2.2 Cervical CancerRecommended Dosage
The recommended dose of Topotecan Injection is 0.75 mg/m2 by intravenous infusion over 30 minutes daily on days 1, 2, and 3; followed by cisplatin 50 mg/m2 by intravenous infusion on day 1 repeated every 21 days (a 21-day course).
Dosage Modification Guidelines
Dosage adjustments for subsequent courses of Topotecan Injection in combination with cisplatin are specific for each drug. See manufacturer’s prescribing information for cisplatin administration and hydration guidelines and for cisplatin dosage adjustment in the event of hematologic toxicity.
In the event of severe febrile neutropenia (defined as <1000 cells/mm3 with temperature of 38°C or 100.4°F), reduce the dose of Topotecan Injection to 0.60 mg/m2 for subsequent courses. Alternatively, in the event of severe febrile neutropenia, administer G-CSF following the subsequent course (before resorting to dose reduction) starting from day 4 of the course (24 hours after completion of administration of Topotecan Injection). If febrile neutropenia occurs despite the use of G-CSF, reduce the dose of Topotecan Injection to 0.45 mg/m2 for subsequent courses. In the event the platelet count falls below 25,000 cells/mm3, reduce doses to 0.60 mg/m2 for subsequent courses. 2.3 Dosage Adjustment in Specific PopulationsRenal Impairment
No dosage adjustment of Topotecan Injection appears to be required for patients with mild renal impairment (Clcr 40 to 60 mL/min.). Dosage adjustment of Topotecan Injection to 0.75 mg/m2 is recommended for patients with moderate renal impairment (20 to 39 mL/min.). Insufficient data are available in patients with severe renal impairment to provide a dosage recommendation for Topotecan Injection. [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)]
Topotecan Injection in combination with cisplatin for the treatment of cervical cancer should only be initiated in patients with serum creatinine ≤1.5 mg/dL. In the clinical trial, cisplatin was discontinued for a serum creatinine >1.5 mg/dL. Insufficient data are available regarding continuing monotherapy with Topotecan Injection after cisplatin discontinuation in patients with cervical cancer.
2.4 Instructions for Handling, Preparation and Intravenous AdministrationHandling
Topotecan is a cytotoxic anticancer drug. Prepare Topotecan Injection under a vertical laminar flow hood while wearing gloves and protective clothing. If Topotecan Injection solution contacts the skin, wash the skin immediately and thoroughly with soap and water. If Topotecan Injection contacts mucous membranes, flush thoroughly with water.
Use procedures for proper handling and disposal of anticancer drugs. Several guidelines on this subject have been published.1-4
Preparation and Administration
The appropriate volume of the Topotecan Injection is diluted in a minimum of 50 mL of 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP prior to administration. Infuse over 30 minutes. Topotecan Injection diluted for infusion is stable for 4 hours at room temperature or 24 hours at refrigerated temperature in ambient lighting conditions.
Topotecan Injection is supplied as a multiple dose vial. Studies have shown the product is stable for 28 days after initial puncture when stored under refrigerated conditions.
-
Teva Parenteral Medicines, Inc.
Topotecan | Teva Parenteral Medicines, Inc.
Verify dose using body surface area prior to dispensing. Recommended dosage should generally not exceed 4 mg intravenously [see Overdosage (10)].
2.1 Small Cell Lung CancerRecommended Dosage: The recommended dose of Topotecan Injection is 1.5 mg/m2 by intravenous infusion over 30 minutes daily on days 1 to 5 of each 21-day cycle until disease progression.
Dosage Modification Guidelines: Recommended dose modifications in patients with bone marrow suppression or renal impairment are provided in the table below [see Warnings and Precautions (5.1), Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
Table 1. Recommended Dose Modifications in Patients with Small Cell Lung Cancer Adverse Reaction or Laboratory Values Recommended Dose ModificationOn Day 1 of first cycle
--neutrophil count of ≤ 1,500 cells/mm3or
--platelet count ≤ 100,000 cells/mm3or
--serum creatinine > 1.5 mg/dL Delay initiation of Topotecan Injection until hematologic or renal recoveryOn Day 1 of subsequent cycles (cycle 2 and beyond)
--neutrophil count of ≤ 1,000 cells/mm3or
--platelet count ≤ 100,000 cells/mm3or
--hemoglobin < 9.0 gm/dL or
--serum creatinine > 1.5 mg/dL Delay next cycle of Topotecan Injection until hematologic or renal recovery For neutropenia < 500 cells/mm3 in preceding cycle Permanently reduce Topotecan Injection dose to 1.25 mg/m2 or administer prophylactic granulocyte colony-stimulating factor during subsequent cycles. For platelets < 25,000 cells/mm3 in preceding cycle Permanently reduce Topotecan Injection dose to 1.25 mg/m2 For creatinine clearance 20-39 mL/min Reduce the Topotecan Injection dose to 0.75 mg/m2 2.2 Cervical CancerRecommended Dosage: The recommended dose of Topotecan Injection is 0.75 mg/m2 by intravenous infusion over 30 minutes daily on days 1, 2, and 3 of each 21-day cycle. Administer cisplatin 50 mg/m2 by intravenous infusion on day 1 of each 21-day cycles.
Dosage Modification Guidelines: Recommended dose modifications in patients with bone marrow suppression or renal impairment are provided in the table below [see Warnings and Precautions (5.1), Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)]. See manufacturer’s prescribing information for cisplatin administration and hydration guidelines and for cisplatin dosage adjustment in the event of hematologic toxicity.
Table 2. Recommended Dose Modifications in Patients with Cervical Cancer Adverse Reaction or Laboratory Values Recommended Dose ModificationOn Day 1 of first cycle
--neutrophil count of ≤ 1,500 cells/mm3or
--platelet count ≤ 100,000 cells/mm3or
--serum creatinine > 1.5 mg/dL Delay initiation of Topotecan Injection until hematologic or renal recoveryOn Day 1 of subsequent cycles (cycle 2 and beyond)
--neutrophil count of ≤ 1,000 cells/mm3or
--platelet count ≤ 100,000 cells/mm3or
--hemoglobin < 9.0 gm/dL or
--serum creatinine > 1.5 mg/dL Delay next cycle of Topotecan Injection until hematologic or renal recovery For the first occurrence of febrile neutropenia [ < 1,000 neutrophils/mm3 with fever ≥ 38.0°C (≥ 100.4°F) in preceding cycle Permanently reduce the daily Topotecan Injection dose to 0.60 mg/m2 or administer prophylactic granulocyte colony-stimulating factor (G-CSF) during subsequent cycles. For re-occurrence of febrile neutropenia [< 1,000 neutrophils/mm3 with fever ≥ 38.0°C (≥ 100.4°F) in preceding cycle despite use of G-CSF Permanently reduce the daily Topotecan Injection dose to 0.45 mg/m2 For platelet nadir < 25,000 cells/mm3 in preceding cycle Permanently reduce the daily Topotecan Injection dose to 0.60 mg/m2 For serum creatinine > 1.5 mg/dL in subsequent cycles Permanently discontinue cisplatin and Topotecan Injection 2.3 Instructions for Handling, and Preparation for Intravenous AdministrationUse procedures for proper handling and disposal of anticancer drugs [see References (15)].
Dilute Topotecan Injection in either 0.9% Sodium Chloride USP or 5% Dextrose USP. Store diluted Topotecan Injection solutions at approximately 20°C to 25°C (68°F to 77°F) for no more than 4 hours or under refrigerated (2°C to 8°C) conditions for no more than 12 hours.
-
Hospira, Inc.
Topotecan | Hospira, Inc.
Verify dose using body surface area prior to dispensing. Recommended dosage should generally not exceed 4 mg intravenously [see Overdosage (10)].
Prior to administration of the first course of Topotecan Injection, patients must have a baseline neutrophil count of >1,500 cells/mm3 and a platelet count of >100,000 cells/mm3.
2.1 Small Cell Lung CancerRecommended Dosage
The recommended dose of Topotecan Injection is 1.5 mg/m2 by intravenous infusion over 30 minutes daily for 5 consecutive days, starting on day 1 of a 21-day course. In the absence of tumor progression, a minimum of 4 courses is recommended because tumor response may be delayed. The median time to response in 4 small cell lung cancer trials was 5 to 7 weeks.Dosage Modification Guidelines
In the event of severe neutropenia (defined as <500 cells/mm3) during any course, reduce the dose by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. Alternatively, in the event of severe neutropenia, administer G-CSF (granulocyte-colony stimulating factor) following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hours after completion of topotecan administration). In the event the platelet count falls below 25,000 cells/mm3, reduce doses by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. 2.2 Dosage Adjustment in Special PopulationsRenal Impairment
No dosage adjustment of Topotecan Injection appears to be required for patients with mild renal impairment (Clcr 40 to 60 mL/min.). Dosage adjustment of Topotecan Injection to 0.75 mg/m2 is recommended for patients with moderate renal impairment (20 to 39 mL/min.). Insufficient data are available in patients with severe renal impairment to provide a dosage recommendation for Topotecan Injection [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
2.3 Instructions for Handling, Preparation and Intravenous AdministrationHandling
Topotecan Injection is a cytotoxic anticancer drug. Prepare topotecan hydrochloride injection under a vertical laminar flow hood while wearing gloves and protective clothing. If Topotecan Injection solution contacts the skin, wash the skin immediately and thoroughly with soap and water. If Topotecan Injection contacts mucous membranes, flush thoroughly with water.
Use procedures for proper handling and disposal of anticancer drugs. Several guidelines on this subject have been published.1-4
Preparation and Administration
The appropriate volume of Topotecan Injection is diluted in a minimum of 50 mL of 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP prior to administration. Infuse over 30 minutes. Topotecan Injection diluted for infusion is stable between 20°C and 25°C (68°F and 77°F) in ambient lighting conditions for 24 hours.
Each vial of Topotecan Injection is intended for single use only. Any unused drug remaining after injection must be discarded.
2.1 Small Cell Lung CancerRecommended Dosage
The recommended dose of Topotecan Injection is 1.5 mg/m2 by intravenous infusion over 30 minutes daily for 5 consecutive days, starting on day 1 of a 21-day course. In the absence of tumor progression, a minimum of 4 courses is recommended because tumor response may be delayed. The median time to response in 4 small cell lung cancer trials was 5 to 7 weeks.Dosage Modification Guidelines
In the event of severe neutropenia (defined as <500 cells/mm3) during any course, reduce the dose by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. Alternatively, in the event of severe neutropenia, administer G-CSF (granulocyte-colony stimulating factor) following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hours after completion of topotecan administration). In the event the platelet count falls below 25,000 cells/mm3, reduce doses by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. 2.2 Dosage Adjustment in Special PopulationsRenal Impairment
No dosage adjustment of Topotecan Injection appears to be required for patients with mild renal impairment (Clcr 40 to 60 mL/min.). Dosage adjustment of Topotecan Injection to 0.75 mg/m2 is recommended for patients with moderate renal impairment (20 to 39 mL/min.). Insufficient data are available in patients with severe renal impairment to provide a dosage recommendation for Topotecan Injection [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
2.3 Instructions for Handling, Preparation and Intravenous AdministrationHandling
Topotecan Injection is a cytotoxic anticancer drug. Prepare topotecan hydrochloride injection under a vertical laminar flow hood while wearing gloves and protective clothing. If Topotecan Injection solution contacts the skin, wash the skin immediately and thoroughly with soap and water. If Topotecan Injection contacts mucous membranes, flush thoroughly with water.
Use procedures for proper handling and disposal of anticancer drugs. Several guidelines on this subject have been published.1-4
Preparation and Administration
The appropriate volume of Topotecan Injection is diluted in a minimum of 50 mL of 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP prior to administration. Infuse over 30 minutes. Topotecan Injection diluted for infusion is stable between 20°C and 25°C (68°F and 77°F) in ambient lighting conditions for 24 hours.
Each vial of Topotecan Injection is intended for single use only. Any unused drug remaining after injection must be discarded.
-
Hospira, Inc.
Topotecan | Hospira, Inc.
Verify dose using body surface area prior to dispensing. Recommended dosage should generally not exceed 4 mg intravenously [see Overdosage (10)].
Prior to administration of the first course of Topotecan Injection, patients must have a baseline neutrophil count of >1,500 cells/mm3 and a platelet count of >100,000 cells/mm3.
2.1 Small Cell Lung CancerRecommended Dosage
The recommended dose of Topotecan Injection is 1.5 mg/m2 by intravenous infusion over 30 minutes daily for 5 consecutive days, starting on day 1 of a 21-day course. In the absence of tumor progression, a minimum of 4 courses is recommended because tumor response may be delayed. The median time to response in 4 small cell lung cancer trials was 5 to 7 weeks.Dosage Modification Guidelines
In the event of severe neutropenia (defined as <500 cells/mm3) during any course, reduce the dose by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. Alternatively, in the event of severe neutropenia, administer G-CSF (granulocyte-colony stimulating factor) following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hours after completion of topotecan administration). In the event the platelet count falls below 25,000 cells/mm3, reduce doses by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. 2.2 Dosage Adjustment in Special PopulationsRenal Impairment
No dosage adjustment of Topotecan Injection appears to be required for patients with mild renal impairment (Clcr 40 to 60 mL/min.). Dosage adjustment of Topotecan Injection to 0.75 mg/m2 is recommended for patients with moderate renal impairment (20 to 39 mL/min.). Insufficient data are available in patients with severe renal impairment to provide a dosage recommendation for Topotecan Injection [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
2.3 Instructions for Handling, Preparation and Intravenous AdministrationHandling
Topotecan Injection is a cytotoxic anticancer drug. Prepare topotecan hydrochloride injection under a vertical laminar flow hood while wearing gloves and protective clothing. If Topotecan Injection solution contacts the skin, wash the skin immediately and thoroughly with soap and water. If Topotecan Injection contacts mucous membranes, flush thoroughly with water.
Use procedures for proper handling and disposal of anticancer drugs. Several guidelines on this subject have been published.1-4
Preparation and Administration
The appropriate volume of Topotecan Injection is diluted in a minimum of 50 mL of 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP prior to administration. Infuse over 30 minutes. Topotecan Injection diluted for infusion is stable between 20°C and 25°C (68°F and 77°F) in ambient lighting conditions for 24 hours.
Each vial of Topotecan Injection is intended for single use only. Any unused drug remaining after injection must be discarded.
2.1 Small Cell Lung CancerRecommended Dosage
The recommended dose of Topotecan Injection is 1.5 mg/m2 by intravenous infusion over 30 minutes daily for 5 consecutive days, starting on day 1 of a 21-day course. In the absence of tumor progression, a minimum of 4 courses is recommended because tumor response may be delayed. The median time to response in 4 small cell lung cancer trials was 5 to 7 weeks.Dosage Modification Guidelines
In the event of severe neutropenia (defined as <500 cells/mm3) during any course, reduce the dose by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. Alternatively, in the event of severe neutropenia, administer G-CSF (granulocyte-colony stimulating factor) following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hours after completion of topotecan administration). In the event the platelet count falls below 25,000 cells/mm3, reduce doses by 0.25 mg/m2 (to 1.25 mg/m2) for subsequent courses. 2.2 Dosage Adjustment in Special PopulationsRenal Impairment
No dosage adjustment of Topotecan Injection appears to be required for patients with mild renal impairment (Clcr 40 to 60 mL/min.). Dosage adjustment of Topotecan Injection to 0.75 mg/m2 is recommended for patients with moderate renal impairment (20 to 39 mL/min.). Insufficient data are available in patients with severe renal impairment to provide a dosage recommendation for Topotecan Injection [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
2.3 Instructions for Handling, Preparation and Intravenous AdministrationHandling
Topotecan Injection is a cytotoxic anticancer drug. Prepare topotecan hydrochloride injection under a vertical laminar flow hood while wearing gloves and protective clothing. If Topotecan Injection solution contacts the skin, wash the skin immediately and thoroughly with soap and water. If Topotecan Injection contacts mucous membranes, flush thoroughly with water.
Use procedures for proper handling and disposal of anticancer drugs. Several guidelines on this subject have been published.1-4
Preparation and Administration
The appropriate volume of Topotecan Injection is diluted in a minimum of 50 mL of 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP prior to administration. Infuse over 30 minutes. Topotecan Injection diluted for infusion is stable between 20°C and 25°C (68°F and 77°F) in ambient lighting conditions for 24 hours.
Each vial of Topotecan Injection is intended for single use only. Any unused drug remaining after injection must be discarded.
![Topotecan Injection, Solution, Concentrate [Teva Parenteral Medicines, Inc.]](http://dailymed.nlm.nih.gov/dailymed/image.cfm?setid=9683e3be-7d23-4ba7-9fe9-9762963604f0&name=42877536-ef36-4b47-9ac8-239055414ea3-03.jpg)
![Topotecan (Topotecan Hydrochloride) Injection, Solution, Concentrate [Hospira, Inc.]](http://dailymed.nlm.nih.gov/dailymed/image.cfm?setid=1d4e1cce-c57e-4a8b-be96-f95a2778e221&name=topotecan1-figure-2-jCA-3052.jpg)
![Topotecan (Topotecan Hydrochloride) Injection, Solution, Concentrate [Hospira, Inc.]](http://dailymed.nlm.nih.gov/dailymed/image.cfm?setid=cc201919-b959-46ce-b0a8-2020e08d500a&name=topotecan-injection2-figure-2-jCA-3195.jpg)
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