Topotecan hydrochloride
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 hydrochloride
- Molecular weight
- 457.91
- Structure (SMILES)
- CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(CN(C)C)c(O)ccc3nc2-1.Cl
- evotopin
- Evotopin
- hycamtin
- Hycamtin
- potactasol
- Potactasol
- topotecan actavis
- Topotecan actavis
- topotecan eagle
- Topotecan eagle
- topotecan hospira
- Topotecan hospira
- topotecan hydrochloride
- Topotecan hydrochloride
- topotecan teva
- Topotecan teva
- 1h pyrano 3 4 6 7 indolizino 1 2 b quinoline 3 14 4h 12h dione 10 dimethylamino methyl 4 ethyl 4 9 dihydroxy monohydrochloride s
- 1H-PYRANO(3',4':6,7)INDOLIZINO(1,2-B)QUINOLINE-3,14(4H,12H)-DIONE, 10-((DIMETHYLAMINO)METHYL)-4-ETHYL-4,9-DIHYDROXY-, MONOHYDROCHLORIDE, (S)-
- evotopin
- Evotopin
- hycamtin
- Hycamtin
- HYCAMTIN
- nogitecan hydrochloride
- Nogitecan hydrochloride
- NOGITECAN HYDROCHLORIDE [JAN]
- nogitecan hydrochloride jan
- nsc 759263
- NSC-759263
- sk f s 104864 a
- sk f s 104864a
- sk s 104864 a
- SK-S-104864-A
- SK&F S-104864-A
- SK&F-S-104864-A
- SK&F-S-104864A
- Topotecan (as hydrochloride)
- topotecan actavis
- Topotecan actavis
- topotecan as hydrochloride
- topotecan hcl
And 21 more, listed on the interactive page.
- CAS registry numbers
- 119413-54-6
- ChEMBL ID
- CHEMBL1607
- InChIKey
- DGHHQBMTXTWTJV-BQAIUKQQSA-N
- RxNorm IDs (RxCUI)
- 266573
- FDA ingredient codes (UNII)
- 956S425ZCY
- 60699
- 11972519
- 57525346
- 172473749
- Applicant
- SANDOZ
- Approval date
- 28 May 1996
- Application number
- NDA020671
- Patents
- 0
- Designations
- 1
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Drug name stem
- -tecan
Administration routes
- Oral
- Parenteral
Mechanisms of action
- Mechanism
- DNA topoisomerase I inhibitor
- Action type
- Inhibitor
- Target
- DNA topoisomerase 1
- Protein identifier
- P11387
Open Targets mechanisms
- Mechanism
- DNA topoisomerase I inhibitor
- Action type
- Inhibitor
- Target
- DNA topoisomerase 1
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Neoplasms, Plasma Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000200
- Subject identifier
- D054219
- Condition
- Carcinoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Carcinoma, Endometrioid
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000466
- Subject identifier
- D018269
- Condition
- Ganglioneuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000502
- Subject identifier
- D018305
- Condition
- Leukemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Neuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000621
- Subject identifier
- D009447
- Condition
- Sarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001061
- Subject identifier
- D002583
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Uterine Cervical Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001416
- Subject identifier
- D002583
- Condition
- Myeloproliferative Disorders
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002428
- Subject identifier
- D009196
- Condition
- Rhabdomyosarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002918
- Subject identifier
- D012208
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Brain Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003833
- Subject identifier
- D001932
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003893
- Subject identifier
- D010051
- Condition
- Carcinoma, Small Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0008524
- Subject identifier
- D018288
- Condition
- Cystadenoma, Serous
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000043
- Subject identifier
- D018293
- Condition
- Central Nervous System Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000158
- Subject identifier
- D016543
- Condition
- Sarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Peritoneal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002087
- Subject identifier
- D010534
And 10 more, listed on the interactive page.
- Condition identifier
- EFO_0000313
- Condition identifier
- EFO_0000565
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000621
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000691
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000702
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003893
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004251
- Highest recorded phase
- 2
- Condition identifier
- EFO_0008524
- Condition identifier
- EFO_1000158
- Highest recorded phase
- 2
- Condition identifier
- HP_0002863
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000402
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0001409
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001416
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002974
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004952
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004993
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005035
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005059
- Highest recorded phase
- 2
And 35 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- hematological toxicity
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Warning
- Black Box Warning
- Effect
- hematological toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- immune system toxicity
- Country
- United States
- Event
- anaemia
- Reports
- 305
- Reporting signal score
- 385.157
- Event
- anaplastic lymphoma kinase gene mutation
- Reports
- 20
- Reporting signal score
- 121.942
- Event
- anorexia
- Reports
- 29
- Reporting signal score
- 46.2519
- Event
- ascites
- Reports
- 59
- Reporting signal score
- 91.9726
- Event
- bone marrow failure
- Reports
- 42
- Reporting signal score
- 51.389
- Event
- bronchospasm
- Reports
- 25
- Reporting signal score
- 29.1621
- Event
- cerebral cyst
- Reports
- 10
- Reporting signal score
- 34.8846
- Event
- chorioretinal atrophy
- Reports
- 22
- Reporting signal score
- 100.766
- Event
- choroidal infarction
- Reports
- 17
- Reporting signal score
- 86.0631
- Event
- decreased appetite
- Reports
- 98
- Reporting signal score
- 58.4281
- Event
- dehydration
- Reports
- 95
- Reporting signal score
- 68.6295
- Event
- desmoplastic small round cell tumour
- Reports
- 16
- Reporting signal score
- 97.7848
- Event
- disease progression
- Reports
- 118
- Reporting signal score
- 132.76
- Event
- enophthalmos
- Reports
- 8
- Reporting signal score
- 35.671
- Event
- febrile bone marrow aplasia
- Reports
- 46
- Reporting signal score
- 128.417
- Event
- febrile neutropenia
- Reports
- 216
- Reporting signal score
- 411.164
- Event
- general physical health deterioration
- Reports
- 59
- Reporting signal score
- 44.2653
- Event
- genotoxicity
- Reports
- 12
- Reporting signal score
- 68.5714
- Event
- haematotoxicity
- Reports
- 53
- Reporting signal score
- 123.407
- Event
- haemoglobin decreased
- Reports
- 72
- Reporting signal score
- 39.7293
- Event
- heterochromia iridis
- Reports
- 7
- Reporting signal score
- 38.8227
- Event
- ileus
- Reports
- 30
- Reporting signal score
- 46.2548
- Event
- iris adhesions
- Reports
- 10
- Reporting signal score
- 32.9469
- Event
- iris atrophy
- Reports
- 17
- Reporting signal score
- 79.2616
- Event
- lenticular opacities
- Reports
- 12
- Reporting signal score
- 45.3665
And 26 more, listed on the interactive page.
- NCT00002537
- NCT00002625
- NCT00003281
- NCT00003812
- NCT00003917
- NCT00003943
- NCT00004055
- NCT00004137
- NCT00004186
- NCT00006012
- NCT00006374
- NCT00025272
- NCT00028925
- NCT00033696
- NCT00041015
- NCT00087048
- NCT00287963
- NCT00365547
- NCT00388089
- NCT00002587
- NCT00002948
- NCT00002950
- NCT00003194
- NCT00003198
- NCT00003331
And 95 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
Conditions of use
- Discard after 24 hours if unused after reconstitution
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 104.89
- Calculated partition coefficient (ALogP)
- 1.85
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 32
- Molecular formula
- C23H24ClN3O5
- Monoisotopic mass
- 457.1404486
- Natural product
- No
- 0078-0674
- 0409-0302
- 16729-151
- 45963-615
- 63323-762
- 66758-101
- 66758-102
- Recorded assays
- 1,986
- Active assays
- 790
- Confirmatory
- Other
- Screening
- Summary
- Topoisomerase I Inhibitors
These details could not be displayed.
Related records
Trials (420)
- 7-hydroxystaurosporine and Topotecan Hydrochloride in Treating Patients With Relapsed or Progressed Small Cell Lung Cancer
- 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 Dose Finding Phase I Trial of the Combination of Topotecan and PS-341, a Novel Proteasome Inhibitor, in Advanced Malignancies
- 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 II/III Study of IBB0979 in Combination With Topotecan Versus Topotecan in Relapsed Small Cell Lung Cancer
- A Phase III Study of BD0801 Combined With Chemotherapy in Recurrent, Platinum-resistant Epithelial Ovarian Cancer
- A Phase III Study of YL201 in Relapsed Small Cell Lung 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
Approved for (8)
- Carcinoma
- Cervical adenocarcinoma
- Cervical cancer
- Cervical carcinoma
- Ovarian cancer
- Ovarian neoplasm
- Small cell carcinoma
- Small cell lung carcinoma
In development for (26)
- Brain neoplasm Phase 1
- Breast cancer Phase 2
- Central nervous system neoplasm Phase 2
- Endometrioid adenocarcinoma Phase 1
- Esophageal cancer Phase 1
- Fallopian tube cancer Phase 3
- Ganglioneuroblastoma Phase 3
- Leukemia Phase 2
- Lung cancer Phase 3
- Lymphoma Phase 2
- Myelodysplastic syndrome Phase 2
- Myeloproliferative neoplasm Phase 1
- Neoplasm Phase 2
- Neuroblastoma Phase 3
- Non-small cell lung carcinoma Phase 3
- Ovarian serous cystadenocarcinoma Phase 1
- Peripheral primitive neuroectodermal tumor Phase 2
- Peritoneum cancer Phase 3
- Plasma cell myeloma Phase 1
- Plasma cell neoplasm Phase 1
Targets (1)
- TOP1 DNA topoisomerase I inhibitor