Topotecan
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1996
- First approval year
- 1996
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Topotecan
- Molecular weight
- 421.45
- Structure (SMILES)
- CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(CN(C)C)c(O)ccc3nc2-1
- 10 hydroxy 9 dimethylamino methyl 20s camptothecin
- 10-HYDROXY-9-((DIMETHYLAMINO)METHYL)-(20S)-CAMPTOTHECIN
- ff 10850 liposomal topotecan
- ff 10850 topotecan liposome injection
- Ff-10850 (liposomal topotecan)
- FF-10850 Topotecan Liposome Injection
- hycamptamine
- Hycamptamine
- hycamptin
- Hycamptin
- nogitecan
- Nogitecan
- nsc 609699
- nsc 641007
- NSC-609699
- NSC-641007
- sk f 104864
- SK&F-104864
- skf 104864
- SKF-104864
- topotecan
- Topotecan
- TOPOTECAN [EMA EPAR]
- topotecan [INN]
- TOPOTECAN [MI]
And 9 more, listed on the interactive page.
- ATC classification codes
- L01CE01
Sources for recorded values
- CAS registry numbers
- 123948-87-8
- ChEMBL ID
- CHEMBL84
- InChIKey
- UCFGDBYHRUNTLO-QHCPKHFHSA-N
- FDA ingredient codes (UNII)
- 7M7YKX2N15
- 60700
- 177494139
- 57308
- 266573
- Applicant
- SANDOZ
- Approval date
- 28 May 1996
- Application number
- NDA020671
- Status
- Authorised
- Status date
- 12 Nov 1996
- Authorisation date
- 12 Nov 1996
- Approved indications
- Hycamtin capsules are indicated as monotherapy for the treatment of adult patients with relapsed small cell lung cancer (SCLC) for whom re-treatment with the first-line regimen is not considered appropriate. Topotecan is indicated for the treatment of patients with metastatic carcinoma of the ovary after failure of first-line or subsequent therapy. Hycamtin capsules are indicated as monotherapy for the treatment of adult patients with relapsed small cell lung cancer (SCLC) for whom re-treatment with the first-line regimen is not considered appropriate.
- Product number
- EMEA/H/C/000123
- Authorisation holder
- Sandoz Pharmaceuticals d.d.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 1
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Ovarian Neoplasms
- Small Cell Lung Carcinoma
- Uterine Cervical Neoplasms
European medicines record
- Patents
- 0
- Designations
- 1
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- topotecan
- Type
- Synthetic organic
- Drug name stem
- -tecan
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
Open Targets mechanisms
- Mechanism
- DNA topoisomerase I inhibitor
- Action type
- Inhibitor
- Target
- DNA topoisomerase 1
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- TOP1MT
- Protein identifier
- Q969P6
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Sarcoma, Ewing
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000174
- Subject identifier
- D012512
- Condition
- Neoplasms, Plasma Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000200
- Subject identifier
- D054219
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Ganglioneuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000502
- Subject identifier
- D018305
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Leukemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Liposarcoma, Myxoid
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000613
- Subject identifier
- D018208
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Neuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000621
- Subject identifier
- D009447
- Condition
- Oligodendroglioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000630
- Subject identifier
- D009837
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001061
- Subject identifier
- D002583
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001416
- Subject identifier
- D002583
- Condition
- Fibrosarcoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002087
- Subject identifier
- D005354
- Condition
- Astrocytoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002499
- Subject identifier
- D001254
- Condition
- Oligodendroglioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002501
- Subject identifier
- D009837
- Condition
- Melanoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Rhabdomyosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002918
- Subject identifier
- D012208
- Condition
- Medulloblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002939
- Subject identifier
- D008527
And 37 more, listed on the interactive page.
- Condition identifier
- EFO_0000220
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000565
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000621
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000681
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000702
- Condition identifier
- EFO_0001061
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001416
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003833
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003893
- Condition identifier
- EFO_0007362
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000453
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000657
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000823
- Highest recorded phase
- 1
- Condition identifier
- EFO_1001331
- Highest recorded phase
- 1
- Condition identifier
- EFO_1001471
- Highest recorded phase
- 1
- Condition identifier
- HP_0001945
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000402
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000448
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001475
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001657
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 3
And 84 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- hematological toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Country
- United States
- Event
- acute myeloid leukaemia
- Reports
- 19
- Reporting signal score
- 29.6585
- Event
- anaemia
- Reports
- 265
- Reporting signal score
- 338.347
- Event
- anaplastic lymphoma kinase gene mutation
- Reports
- 12
- Reporting signal score
- 68.8985
- Event
- anorexia
- Reports
- 21
- Reporting signal score
- 30.0627
- Event
- ascites
- Reports
- 50
- Reporting signal score
- 77.7242
- Event
- bone marrow failure
- Reports
- 41
- Reporting signal score
- 55.0009
- Event
- bronchospasm
- Reports
- 25
- Reporting signal score
- 32.8972
- Event
- cerebral cyst
- Reports
- 8
- Reporting signal score
- 27.3071
- Event
- chorioretinal atrophy
- Reports
- 19
- Reporting signal score
- 87.2055
- Event
- choroidal dystrophy
- Reports
- 6
- Reporting signal score
- 28.9903
- Event
- choroidal infarction
- Reports
- 13
- Reporting signal score
- 64.3539
- Event
- cutaneous lupus erythematosus
- Reports
- 11
- Reporting signal score
- 24.5844
- Event
- decreased appetite
- Reports
- 78
- Reporting signal score
- 42.1581
- Event
- dehydration
- Reports
- 71
- Reporting signal score
- 44.0535
- Event
- desmoplastic small round cell tumour
- Reports
- 16
- Reporting signal score
- 100.289
- Event
- disease progression
- Reports
- 114
- Reporting signal score
- 140.783
- Event
- enophthalmos
- Reports
- 7
- Reporting signal score
- 31.3698
- Event
- febrile bone marrow aplasia
- Reports
- 44
- Reporting signal score
- 127.89
- Event
- febrile neutropenia
- Reports
- 162
- Reporting signal score
- 287.349
- Event
- general physical health deterioration
- Reports
- 55
- Reporting signal score
- 45.0599
- Event
- genotoxicity
- Reports
- 12
- Reporting signal score
- 70.4474
- Event
- haematotoxicity
- Reports
- 43
- Reporting signal score
- 97.9092
- Event
- haemoglobin decreased
- Reports
- 59
- Reporting signal score
- 30.9121
- Event
- heterochromia iridis
- Reports
- 7
- Reporting signal score
- 39.9156
- Event
- ileus
- Reports
- 24
- Reporting signal score
- 35.5932
And 30 more, listed on the interactive page.
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And 170 more, listed on the interactive page.
- Dose
- 1.5 mg/m2
- Route
- Intravenous
- How often
- Daily for 5 consecutive days starting on Day 1 of a 21-day cycle
- Do not administer subsequent cycles until neutrophils recover to >1000/mm3, platelets to >100,000/mm3, hemoglobin to ≥9 g/dL
- Do not exceed a single dose of 4 mg
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 104.89
- Calculated partition coefficient (ALogP)
- 1.85
- Calculated partition coefficient (XLogP)
- 0.5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 31
- Molecular formula
- C23H23N3O5
- Monoisotopic mass
- 421.16377084
- Natural product
- Yes
- 16729-243
- Recorded assays
- 4,928
- Active assays
- 1,027
- Confirmatory
- Other
- Screening
- Topoisomerase I Inhibitors
These details could not be displayed.
Related records
Trials (264)
- 9-ING-41 in Pediatric Patients With Refractory Malignancies.
- A Bioequivalence Study of Two Oral Formulations of Topotecan in Patients With Advanced Solid Tumors
- A Multi-Arm, Platform Trial For Relapsed Neuroblastoma
- a Multicenter Clinical Trial for the Treatment of Children and Adolescents With Soft Tissue Sarcoma Stage 4
- A Pharmacokinetic Study of Oral Cyclophosphamide and Topotecan in Children With Recurrent Solid Tumors
- A Phase 1b Study of Sevacizumab in Combination With Chemotherapy in Chinese Patients With Platinum-Resistant Recurrent Ovarian Cancer.
- A Phase 2 Study Comparing TAS-102 Versus Topotecan or Amrubicin to Treat Small Cell Lung Cancer Following Platinum-Based Chemotherapy
- A Phase I Study of CCI-779 (Temsirolimus) in Combination With Topotecan in Patients With Gynecologic Malignancies
- A Phase I Study of Oral Topotecan as a Radiosensitizing Agent in Patients With Rectal Carcinoma
- A Phase I Topotecan Study in Subjects With Cancer and Impaired Renal Function
- A Phase I/II Study of Induction Chemotherapy With Daunorubicin, Cytarabine, Topotecan and Etoposide
- A Phase II Study of Paclitaxel and Topotecan With Filgrastim-SD/01 Support For Relapsed and Refractory Aggressive Non-Hodgkin's Lymphoma
- A Phase II Study of Topotecan in Children With Recurrent Wilms Tumor
- A Phase III Study of BD0801 Combined With Chemotherapy in Recurrent, Platinum-resistant Epithelial Ovarian Cancer
- A Pilot Trial of Oral Topotecan for the Treatment of Refractory Advanced Solid Neoplasms Expressing HIF-1a
- A Prospective International Multicenter Clinical Trial for Eyes With Relapsed Retinoblastoma
- A Randomized Study to Compare the Efficacy and Safety of Belotecan and Topotecan as Monotherapy for Sensitive-Relapsed Small Cell Lung Cancer
- A Study Comparing BL-B01D1 With Topotecan in Patients With Recurrent Small Cell Lung Cancer(PANKU-Lung03)
- A Study Comparing BL-M07D1 With Physician's Choice of Chemotherapy in Patients With HER2-Expressing Platinum-Resistant Recurrent Epithelial Ovarian Cancer, Fallopian Tube Cancer, and Primary Peritoneal Cancer
- A Study Evaluating BSI-201 in Combination With Chemotherapeutic Regimens in Subjects With Advanced Solid Tumors
Approved for (1)
In development for (104)
- Acute leukemia Phase 2
- Acute lymphoblastic leukemia Phase 3
- Acute myeloid leukemia Phase 2
- Adrenal cortex neoplasm Phase 1
- Anaplastic astrocytoma Phase 1
- Anaplastic oligodendroglioma Phase 1
- Aseptic meningitis Phase 1
- Astrocytic tumor Phase 1
- Astrocytoma (excluding glioblastoma) Phase 2
- Atypical choroid plexus papilloma Phase 1
- Atypical teratoid rhabdoid tumor Phase 2
- B-cell chronic lymphocytic leukemia Phase 1
- Brain cancer Phase 2
- Brain neoplasm Phase 2
- Brain stem glioma Phase 1
- Breast neoplasm Phase 2
- Cancer Phase 3
- Central nervous system cancer Phase 2
- Central nervous system neoplasm Phase 2
- Cervical adenocarcinoma Phase 3
Other linked conditions (1)
- Primary central nervous system lymphoma