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Topotecan hydrochloride

Chemical Name:
Topotecan hydrochloride
HYDROCHLORIDE;Hycamtin;TOPOTECAN HCL;2-(3-Chloro-5-trifluoromethyl-pyridin-2-yl)-ethylamine;108563;NSC 609669;Levulan-13C;SKF-104864A;SKFS 104864A;Nogitecan HCl
Molecular Formula:
Molecular Weight:
MDL Number:
MOL File:
Last updated:2024-09-07 18:57:57

Topotecan hydrochloride Properties

Melting point 213-218°C
storage temp. Sealed in dry,Room Temperature
solubility DMSO (Slightly), Methanol (Slightly), Water (Slightly)
form Light yellow to greenish powder.
color White to Off-White
Stability Hygroscopic
CAS DataBase Reference 119413-54-6(CAS DataBase Reference)
NCI Dictionary of Cancer Terms ;
NCI Drug Dictionary


Risk and Safety Statements

Symbol(GHS)  trực tiếp đá gà hôm nayLiên kết đăng nhập
Signal word  Danger
Hazard statements  H351-H340-H361
Precautionary statements  P201-P202-P281-P308+P313-P405-P501-P201-P202-P281-P308+P313-P405-P501
Hazard Codes  T
Risk Statements  25-36/37/38-46
Safety Statements  26-36/37/39-45
HS Code  29420000
NFPA 704
4 0

Topotecan hydrochloride price More Price(61)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 14129 Topotecan (hydrochloride) ≥98% 119413-54-6 5mg $31 2025-03-01 Buy
Cayman Chemical 14129 Topotecan (hydrochloride) ≥98% 119413-54-6 10mg $43 2025-03-01 Buy
Cayman Chemical 14129 Topotecan (hydrochloride) ≥98% 119413-54-6 25mg $96 2025-03-01 Buy
Cayman Chemical 14129 Topotecan (hydrochloride) ≥98% 119413-54-6 50mg $177 2025-03-01 Buy
Tocris 4562 Topotecanhydrochloride ≥98%(HPLC) 119413-54-6 50 $210 2022-12-16 Buy
Product number Packaging Price Buy
14129 5mg $31 Buy
14129 10mg $43 Buy
14129 25mg $96 Buy
14129 50mg $177 Buy
4562 50 $210 Buy

Topotecan hydrochloride Chemical Properties,Uses,Production

Anticancer drug

Topotecan hydrochloride is a water-soluble derivative of camptothecin, which is the form of hydrochloride of topotecan. It is successfully developed by the SmithKline Beecham US company, and approved by the FDA in the United States in 1996. Its trade name is Hycamtin. It is applied in the treatment of ovarian cancer (OVC) as the second-line therapy.
In 1999 the US Food and Drug Administration (FDA) has approved topotecan hydrochloride as small cell lung cancer (SCLC) therapeutic drug. It has been available in the UK, Germany, France and other dozens of countries and regions. The Ⅲ clinical trials are ongoing for this medicine which is used to treat non-small cell lung cancer, cervical cancer, myelodysplastic syndrome.
Topotecan hydrochloride can enter the blood brain barrier. It has the same effect of oral and intravenous injection. The drug has low toxicity predictable bone marrow suppression, and other minor non-hematologic toxicity. Currently there are manufacturers, for clinical treatment of small cell lung cancer, ovarian cancer and other tumors.
Topotecan hydrochloride inhibits the activity of topoisomerase I, which is required for DNA replication. After intravenous injection, the product is hydrolyzed in the blood, and excreted by urinary. This product has a rapid serum clearance rate, which is 62L/h. It is widely distributed in vivo, and Its half-lifetime is about 2~3h. Preclinical trials have shown that the product has anti-tumor activity on all kinds of types of tumor. In I clinical trial, to patients with ovarian cancer that is cisplatin tolerance, this product also has significant anti-tumor effect.

Clinical studies

In a open randomized trial, 226 cases who used cisplatin or carboplatin invalid or recurrent advanced ovarian cancer women changed to this product, and compared with paclitaxel. In 112 patients who used topotecan hydrochloride, 22 cases were effective, so the effective rate was 20%. In 114 patients treated with paclitaxel, 14 cases were effective, so the effective rate was 12%. Used this product for treatment which has made significant improvement in the average time of 23 weeks, while 14 weeks for paclitaxel. In a non-controlled trial to 111 women patients with refractory advanced ovarian cancer, 16 cases were preferabe after treatment, occupied with 14%, and the curative effect average time was 16-week, and the average survival time was 52-week. In an open trial, 67 cases were ineffective treated with cisplatin and paclitaxel for advanced ovarian cancer. However, 9 cases who changed to this product were effective, and the effective rate was 13%.
The above information is edited by the chemicalbook of Kui Ming.

Side effects

It can appear toxicity of bone marrow suppression in limited doses, especially it can cause neutropenia. It often induced thrombocytopenia and anemia. Sometimes red blood cell and platelet transfusion is necessary. It can also be nausea, vomiting, hair loss, diarrhea, abdominal pain, gastritis and weakness, but all of them were mild.


It is used as antineoplastic agent.


Topotecan is a chemotherapeutic agent medication and acts as a topoisomerase inhibitor. Topotecan is asynthetic, water-soluble analog of camptothecin. It is used in the form of its hydrochloride salt to treat ovarian cancer, lung cancer and other cancer types.

Chemical Properties

White Crystalline Solid


Hycamtin,SmithKline Beecham Pharmaceuticals,UK


antineoplastic; topoisomerase I inhibitor


Naturally occurring amino acid; precursor of tetrapyrroles in the biosynthesis of chlorophyll and heme. Antineoplastic (photosensitizer)


A DNA topoisomerase I inhibitor; semisynthetic analog of Camptothecin. Antineoplastic. Topotecan hydrochloride is a chemotherapy agent that is a topoisomerase 1 inhibitor.

Manufacturing Process

Camptothecin (CPT) - a compound isolated from the bark, leaves and fruit of Camptotheca acuminate (Wall M. E. et al., J. Am. Chem. Soc. 88, 3888, 1966).
10-Hydroxycamptothecin (10-HCPT) was prepared by subjecting CPT (3.2 g 0.0092 mol), 0.8 g of Pt0 (prepared by pre-reduction of 8 g of amorphous PtO2 in 80 ml of acetic acid for 1.5 h under 1 atm hydrogen pressure) and acetic acid to 1 atm of H2 for 8.5 h after which theoretical amount of H2 absorbed (slightly more than 0.4 L) and uptake of H2 gets slowed down. The reaction mixture was degassed under steam of helium and filtered through celite and washed with acetic acid (20 ml). The resulting solution was treated immediately with Pb(OAc)4 (6.4 g 0.014 mol) in portions and reaction mixture, stirred vigorously under helium for 30 min. Gumy residue was obtained on evaporation of solvent which was triturated with cold water (100 ml) to produce light brown solid. The solid was collected, washed with cold water and air dried overnight when a mixture of 10-HCPT (44%), acetyl 10- hydroxycamptothecin (10-AcHCPT, 26%) and unreacted CPT (32%) on HPLC basis was obtained. This crude mixture was combined with 150 ml of 50% acetic acid and heated under reflux conditions overnight. The reaction mixture was cooled, concentrated to 20 ml and treated with cold water (100 ml) to produce precipitate, which is filtered, washed with more cold water and dried to afford 2.1 g of solid containing 10-HCPT (70%), 10-AcCPT (1.2%) and CPT (21.3%) on the basis HPLC. Mixture was triturating with 0.5% aq HCl to dissolve the water-soluble. When insoluble CPT was removed by filtration. Water-soluble was extracted with chloroform and crystallized from boiling solution of 20% of MeOH in CHCl3 by adding EtOAC dropwise until turbidity appeared to obtain pure yellow 10-(HCPT), melting point 268°-270°C. 10-HCPT (0.364 g 0.01 mmol) and 40% aqueous dimethylamine (12 ml) was added in dichloromethane (50 ml) in which anhydrous potassium carbonate (2.17 g, 15 mmol) has been suspended. The reaction mixture was stirred at room temperature for 5 h, then filtered and solid extracted with ethylacetate (20 ml). The solvent is evaporated in vacuo giving a residue. The residue was triturated with 0.5% aq HCl (50 ml) to dissolve the water-soluble adduct. Water-soluble were partitioned with petroleum ether (3 times 50 ml) and followed by ethylacetate (3 times 50 ml). The aqueous layer was lyophilized as an off white hydrochloride salt of 9-[(dimethylamino)methyl]10- hydroxy(20S)-camptothecin (topotecan hydrochloride) yield 0.236 g (65%).

brand name

Topotecan is INN and BAN.

Therapeutic Function


General Description

Topotecan is supplied in 4-mg vials and administered IV forthe treatment of ovarian cancer, cervical cancer, and smallcell lung cancer in those patients who did not respond tofirst-line therapy. Following IV administration, the drug iswidely distributed with 10% to 35% of the agent bound toplasma proteins. There is evidence that the agent may crossthe blood-brain barrier to some extent. In plasma, an equilibriumis established between the lactone and the less activehydroxy acid with 20% of the drug present as the lactone 1hour after the infusion is complete. In contrast to irinotecan,both the lactone and the hydroxy acid bind equally well tohuman serum albumin. N-Demethylation of the tertiaryamine to give the secondary amine is mediated by CYP3A4and represents a minor route of metabolism. Glucuronidationof the parent and the phase I metabolites also occurs to a limited(10%) extent.Elimination occurs primarily in theurine, with 30% of the dose being recovered as unchangeddrug. The terminal elimination half-life is 2 to 3 hours. Themajor toxicity seen for topotecan is dose-limiting myelosuppression.Nausea and vomiting are seen in most (70%–80%)patients, along with diarrhea and abdominal pain. Other toxicitiesinclude headache myalgias, alopecia and elevation ofserum transaminases, alkaline phosphatases, and bilirubin.Microscopic hematuria (blood in the urine) may also be seen.

Biological Activity

topotecan hcl(skf104864)is an inhibitor of topoisomerase 1 and semisynthetic analogue of camptothecin [1].topotecan hcl(skf104864)has been reported to have a potent antitumor activity against tumors in murine models. in addition, topotecan hcl has also shown the potent effect against intravenously implanted p388 leukemia and both intravenously and subcutaneously implanted lewis lung carcinoma. topotecan hcl has noted the activity against subcutaneously implanted solid tumors including chemorefractory tumors and human colon carcinoma xenograft ht-29. topotecan hcl has been found to induce regressions in the lung tumor model (lewis lung carcinoma and b16 melanoma), compared to camptothecin and 9-amino-camptothecin. in the preclinical toxicology studies, topotecan hcl has been revealed to have a concentration-dependent, reversible and limited toxoicity to rapidly proliferation tissues such as bone marrow and gastro-intestinal epithelium [1].


Topotecan elimination is biphasic, with a terminal half-life of 2.0 to 3.5 hours. Lactone hydrolysis is rapid, and binding to serum proteins is limited to between 25 and 40%. CYP3A4-mediated N-dealkylation to mono?and didealkylated metabolites occurs to a limited extent, and the O-glucuronides that form at multiple points along the metabolic path are excreted via the kidney.

Clinical Use

This active camptothecin analogue is used by the IV route in the treatment of ovarian and small cell lung cancer that has not responded to first-line therapy.


Store at -20°C


[1] creemers gj1, lund b, verweij j. topoisomerase i inhibitors: topotecan and irenotecan. cancer treat rev. 1994 jan;20(1):73-96.

Topotecan hydrochloride Preparation Products And Raw materials

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View Lastest Price from Topotecan hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
trực tiếp đá gà hôm nayLiên kết đăng nhập 2024-11-08 Topotecan hydrochloride
US $0.00 / kg 1kg 99% 2000ton Shaanxi Haibo Biotechnology Co., Ltd
trực tiếp đá gà hôm nayLiên kết đăng nhập 2024-11-01 Topotecan hydrochloride
US $0.00-0.00 / kg 1kg 99% 20 tons Hangzhou ICH Biofarm Co., Ltd
trực tiếp đá gà hôm nayLiên kết đăng nhập 2024-08-29 Topotecan hydrochloride
US $0.00 / KG 1KG 99% 50000KG/month Hebei Mojin Biotechnology Co., Ltd

Topotecan hydrochloride Spectrum

1,4-di(4-benzhydryloxy-2-butynyl)piperazine 1,4-di(4-benzyloxy-2-butynyl)piperazine (S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-(H-Pyrano[3' , 4':6,7]indolizino[1,2-b]quinoline-3,14[4H,12H]-dione monohydrochloride Topotecan Hydrochloride(TPT) S-(6-thioxo-1,6-dihydro-pyrimidin-4-yl)-isothiourea Topotecan hydrochloride(NSC-609699) Topotecan, Hydrochloride Salt Toputecan hydrochloride 2-Methyl-4-piperidino-butan-2-ol Topotecan HCl (HycaMtin) 3-Methoxy-5-Methyl-4-MethylaMino-heptanoic acid tert-butyl ester Nogitecan hydrochloride Topotecan hydrochloride (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 hydrochloride 2-Aza-bicyclo[4.1.0]heptane(HCl):2-Aza-bicyclo[4.1.0]heptane (4S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, hydrochloride (1:1) Nogitecan HCl Topotecan Hydrochloride Labeled d6 Topotecan hydrochloride, >=99% N-(oxolan-2-ylmethyl)-2-(propan-2-ylamino)acetamide 2-[5-(1-ethylpyrazol-4-yl)-1,3,4-oxadiazol-2-yl]ethanamine (1S,5R)-3,3-difluoro-8-azabicyclo[3.2.1]octane 5-ALA HCl-13C 5-Amino-4-oxopentanoic Acid-13C 5-Aminolevulinic Acid-3-13C Hydrochloride Aminolevulinic-13C Acid Hydrochloride d-Aminolevulinic-13C Acid Hydrochloride Levulan-13C 9-[(DIMETHYLAMINO)METHYL]-10-HYDROXY-(20S)-CAMPTOTHECIN, HCL (4S)-10-[(DIMETHYLAMINO)METHYL]-4-ETHYL-4,9-DIHYDROXY-1H-PYRANO[3',4',6-7]INDOLIZINO[1,2-B]QUINOLINE-3,14(4H,12H)-DIONE topetecan hydrochloride 5-PIPERAZIN-1-YL-BENZOFURAN-2-CARBOXYLIC ACID ETHYL ESTER (4S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[346-7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, Hydrochloride, SKF-104864A, 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, (4S)- (9CI) 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)- NSC 609669 SKFS 104864A SKF-S 104864-A TOPOTECAN MONOHYDROCHLORIDE SKF-104864A Topotecan Hydrochloride(TECANS) (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 monohydrochloride (4S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3’,4’,6-7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione Hydrochloride 1,4-di[4-(3-phenoxypropoxy)-2-butynyl]piperazine 4,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinoline 1-Methyl-2-(3-methyl-pyrazol-1-yl)-ethylamine 1-Methyl-4-(toluene-4-sulfonyl)-piperazine Benzyl-[1-(2-chloro-ethyl)-piperidin-3-yl]-amine 1,1-Dimethyl-2-(2-oxo-2-phenyl-ethyl)-isothiourea (2S)-2-[[(2R)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanamide (3,5-Dimethoxy-phenyl)-(1H-pyrazol-3-ylmethyl)-amine Topotecan (Nogitecan) HCl Topotecan hydrocloride [2-(4-Methyl-piperazin-1-yl)-ethyl]-carbamic acid tert-butyl ester 5-bromo-7-methoxy-1,2,3,4-tetrahydroisoquinoline-4,6-diol 8-methoxy-7-methyl-3,4-dihydroisoquinoline TOPOTECAN HYDROCHLORIDE 99% (2R)-2-amino-3-(3-methylimidazol-4-yl)propanoic acid
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