Topotecan

This page contains recent news articles, when available, and an overview of Topotecan but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.


Overview:

Topotecan
(when available)

Pharmacology and use:
Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. Topotecan interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other effects may also occur. Unlike irinotecan, topotecan is found predominantly in the inactive carboxylate form at neutral pH and it is not a prodrug. For the treatment of metastatic carcinoma of the ovary and small cell lung cancer following the failure of first-line chemotherapy.

Mechanism Of Action:
Topotecan has the same mechanism of action as irinotecan. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. The cytotoxicity of topotecan is thought to be due to double strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topotecan, topoisomerase I and DNA. Mammalian cells cannot efficiently repair these double strand breaks.

News Articles on Topotecan

Topotecan Combo No Extra Help in Ovarian Cancer  -  Jul 28, 2008
By David Douglas NEW YORK JUL 28, 2008 (Reuters Health) - In women with recurrent ovarian cancer, treatment with topotecan along with etoposide or Cancerpage.com,

Poniard Pharmaceuticals – Platinum Rediscovered (Part II)  -  Jun 22, 2008
Topotecan was originally approved as an IV treatment, but recently, an oral version of the drug received FDA approval, after showing comparable activity. istockAnalyst.com,

Aptuit Consulting Inc. and Taiwan Liposome Company (TLC ...  -  Jun 25, 2008
Lipotecan ® is structurally related to topotecan and other camptothecins, but has been chemically modified to improve stability and potency and to minimize Business Wire (press release),

SUMMIT, NJ, Jun 02, 2008 (BUSINESS WIRE) --  -  02 Jun 2008
Results of the studies demonstrated improved overall response rates that compare favorably with topotecan, as well as no evidence of anthracycline-induced Stockhouse,

Market Report -- In Play (CELG)  -  02 Jun 2008
...primary endpoint of the study was met Results of the studies demonstrated improved overall response rates that compare favorably with topotecan, MSN Money

GSL Receives Authorisation In Europe For Oral Hycamtin(R ...  -  May 13, 2008
GlaxoSmithKline (GSK) announced that oral Hycamtin® (topotecan hard capsules) have received approval from the European Commission for the treatment of Medical News Today (press release),

Topotecan Approved in Europe for Treatment of Relapsed Small-Cell ...  -  May 13, 2008
NEW YORK -- May 13, 2008 -- Oral topotecan (Hycamtin) hard capsules have been approved by the European Commission for the treatment of relapsed small-cell DG News

GlaxoSmithKline Granted European Approval for Lung Cancer Drug  -  May 13, 2008
The approval was based on positive results from a Phase III study comparing topotecan hard capsules plus best supportive care (BSC ) to BSC alone in RedOrbit,

Oncolin Therapeutics Announces That Dr. Randall K. Johnson Has ...  -  May 5, 2008
Among the many accomplishments during his tenure was the development of Topotecan which continues to be a major drug used in cancer therapy today. Business Wire (press release),

Leave your tributes to Mel aka DJ Lucy*Fur  -  May 6, 2008
And Mel was now also faced with having to undergo a more aggressive chemotherapy called Topotecan and Radiotherapy. After continuing with the treatment Whitby Today,

Poniard Pharmaceuticals, Inc. Q1 2008 Earnings Call Transcript  -  May 24, 2008
...docetaxel, liposomal doxorubicin, gemcitabine, topotecan, 5FU and leucovorin, and vinorelbine. Poniard is currently studying the intravenous formulation Seeking Alpha,

BiPar Sciences Announces Clinical Data Presentations on Lead PARP ...  -  May 15, 2008
BiPar will also present a Phase 1b study evaluating BSI-201 in combination with topotecan, gemcitabine, temozolomide and carboplatin/paclitaxel in subjects PR Newswire (press release),

BSI-201 Demonstrates Significant Tumor Growth Inhibition and ...  -  Apr 14, 2008
In combination with topotecan, BSI-201 significantly inhibited tumor growth and increased the percentage of complete tumor regressions, compared with Earthtimes,

GlaxoSmithKline Reports Further Progress of Oncology Portfolio  -  Apr 22, 2008
S-Hall A1 Small Cell Lung Cancer -- Topotecan (HYCAMTIN)/cisplatin (TP) compared to cisplatin/etoposide (PE) for patients with extensive disease-small Earthtimes,

Chemotherapy has roots in herbs  -  Mar 26, 2008
...alkaloids for malignant lymphomas are from periwinkle and the anti-cancer drugs topotecan and irinotecan are extracted from a Chinese Happy Tree component. PRESS TV,

Tekmira Pharmaceuticals Releases 2007 Audited Operating Results  -  Mar 31, 2008
Marqibo(R) (Optisomal Vincristine), Alocrest(TM) (formerly INX-0125, Optisomal Vinorelbine) and Brakiva(TM) (formerly INX-0076, Optisomal Topotecan). FOXBusiness

Chemotherapy Combinations May Benefit, If Ratios Are Controlled  -  Apr 15, 2008
..."When we combined our drug with topotecan, a chemotherapy agent that attacks cancer growth by creating DNA damage in cancer cells, for example, eMaxHealth.com,

BiPar Sciences Expands Clinical Program for BSI-201, a Novel DNA ...  -  Apr 10, 2008
The abstract, "Activity of BSI-201, a potent poly (ADP-ribose) polymerase (PARP) inhibitor, alone and in combination with topotecan in human ovarian Earthtimes,

Gene Expression Signatures Can Refine Breast Cancer Prognosis  -  Apr 1, 2008
...were resistant to cyclophosphamide, docetaxel, and fluorouracil; and patients with poor prognosis were resistant to docetaxel, etoposide, and topotecan. Medscape (subscription)

Myelosuppression: A Report from the 2007 International MASCC/ISOO ...  -  Mar 28, 2008
...thrombocytopenia occurred in 50% of patients who were treated with lenalidomide, azacitidine, or a combination of idarubicin, cytarabine and topotecan. Cancer Consultants,

Thalidomide Shows Promise For Treatment Of Recurrent Ovarian ...  -  Feb 27, 2008
The study compared the effectiveness and safety of the combination of thalidomide and topotecan, a chemotherapy often used for ovarian cancer, Science Daily (press release)

Thalidomide may treat ovarian cancer  -  Feb 28, 2008
His study looked at the effectiveness and safety of using a combination of thalidomide and topotecan, a type of chemotherapy often used for ovarian cancer. Irish Health,

Thalidomide For Recurrent Ovarian Cancer Improves Response  -  Feb 29, 2008
NEW YORK FEB 28, 2008 (Reuters Health) - The addition of thalidomide to topotecan appears to improve treatment response rates of recurrent epithelial Cancerpage.com,

Thalomid® Improves Response to Hycamtin® for Recurrent Ovarian Cancer  -  Mar 4, 2008
Researchers from the University of Minnesota have reported that the addition of Thalomid® (thalidomide) to Hycamtin® (topotecan) improves response rate in Cancer Consultants,

Recurrent Low-grade Carcinoma Of The Ovary Less Responsive To ...  -  Mar 10, 2008
No response was observed in women with platinum-resistant disease to standard chemotherapy agents such as liposomal doxorubicin; topotecan; Science Daily (press release)

BioNumerik Conducts Comparative Trial With Karenitecin  -  Feb 12, 2008
The randomized, multicenter, open-label trial will compare Karenitecin with Hycamtin (topotecan) in patients who have become resistant to platinum and FDA news (subscription),

Hana Biosciences Announces Top-Line Phase 1 Clinical Trial Data ...  -  Feb 12, 2008
Hana's Optisome pipeline includes Marqibo(r) (vincristine), Alocrest(tm) (vinorelbine) and Brakiva(tm) (topotecan). Hana Biosciences, Inc. (Nasdaq:HNAB) is FOXBusiness

Traditional Medicine: Identifying Potential Cancer Treatments Of ...  -  Mar 4, 2008
The modern anti-cancer drugs topotecan and irinotecan are derived from a constituent of the Chinese Happy Tree. Looking for new compounds, Science Daily (press release)

Once-feared Thalidomide may treat ovarian cancer  -  Feb 27, 2008
In the latest study, Downs and his colleagues gave thalidomide and a standard chemotherapy drug (topotecan) to one group of 30 ovarian cancer patients, Houston Chronicle,

Eric K. Rowinsky Joins ADVENTRX Board of Directors  -  Feb 26, 2008
...and preclinical investigations which led to the development of paclitaxel, docetaxel, topotecan, irinotecan, erlotinib and gefitinib, among others. FOXBusiness

SuperGen Reports 2007 Fourth Quarter and Annual Financial Results  -  Mar 3, 2008
...with several standard of care chemotherapy regimens, including carboplatin/paclitaxel, carboplatin/etoposide, docetaxel, topotecan, and erlotinib. Earthtimes,

BioNumerik Commences Global Phase III Ovarian Cancer Trial on ...  -  07 Feb 2008
Either Karenitecin or topotecan will be given intravenously daily for 5 consecutive days repeated every 3 weeks to advanced ovarian cancer patients who have PR Newswire (press release),

GlaxoSmithKline gets EMEA positive opinion for Hycamtin  -  Feb 4, 2008
Topotecan capsules will be indicated as monotherapy for the treatment of adult patients with relapsed small cell lung cancer (SCLC) for whom re-treatment MarketWatch

EU agency backs Glaxo's Hycamtin for lung cancer  -  Feb 4, 2008
The drug, also known as topotecan, will be approved as monotherapy in adult patients for whom re-treatment with the first-line regimen is not considered Reuters UK,

GSK signs $425 million respiratory deal with Amira  -  Feb 5, 2008
GSK also announced that the European Medicines Agency has issued a positive opinion on Hycamtin (topotecan) as a monotherapy for the treatment of relapsed Pharma Times (subscription),

Pharmion's Amrubicin Shows Encouraging Results Compared to ...  -  Nov 9, 2007
The trial presented today compares Amrubicin and topotecan in patients with ED-SCLC that initially responded to first-line platinum-based therapy but whose CNNMoney.com

Pharmion Announces Results in Amrubicin Study  -  Nov 12, 2007
The trial compared Amrubicin and topotecan in patients with extensive-disease small cell lung cancer who initially responded to first-line platinum-based FDA news (subscription),

Hana Biosciences Presents Positive Preclinical Data for Three Anti ...  -  Oct 25, 2007
Abstract #C113 - "A pharmacokinetic study of a novel sphingomyelin/cholesterol liposomal topotecan and nonliposomal topotecan in rats. CNNMoney.com

Pharmion Initiates Pivotal Phase 3 Study of Amrubicin in Small ...  -  Oct 19, 2007
The randomized, controlled, multi-center study will compare amrubicin to topotecan, the only approved chemotherapyterm for second-line treatment of SCLC in Cancer Focus,

Hana Biosciences Presents Positive Preliminary Phase 1 Clinical ...  -  Oct 23, 2007
Hana's Optisome pipeline includes Marqibo(r) (vincristine), Alocrest(tm) (vinorelbine) and Optisomal topotecan. Hana Biosciences, Inc. (Nasdaq:HNAB) is a CNNMoney.com

Tekmira Pharmaceuticals Releases Third Quarter 2007 Operating Results  -  Nov 14, 2007
A Phase 1 trial by Hana investigating Brakiva TM (topotecan hydrochloride injection, OPTISOME TM ; formerly INX-0076) as a treatment for solid tumors. Market Wire (press release)

Pharmion Corporation Reports 2007 Third Quarter Operating Results  -  Oct 31, 2007
The randomized, controlled, multi-center study will enroll patients with sensitive or refractory disease and compare Amrubicin to topotecan, CNNMoney.com

otcpicks.com: otcpicks.com Daily Market Movers Digest Midday ...  -  Oct 31, 2007
...and Sphingosome encapsulated topotecan for the treatment of metastatic carcinoma of the ovary after failure of initial or subsequent chemotherapy, Trading Markets (press release),

Hana Biosciences Receives $30 Million  -  Oct 31, 2007
...(topotecan hydrochloride injection, OPTISOME?) this year. For Menadione, Hana?s supportive care product candidate, the company plans to submit an Ad-Hoc-News (Pressemitteilung),

Tekmira Partner Hana Biosciences Achieves Clinical Progress in 2007  -  Oct 23, 2007
...and for product candidates Marqibo ® (vincristine sulfate injection, OPTISOME TM ), and Brakiva TM (topotecan hydrochloride injection, OPTISOME TM ). Market Wire (press release)

Antiemetics, Their Function, and Their Role in Controlling ...  -  Oct 18, 2007
Low-risk drugs are paclitaxel, docetaxel, mitoxantrone, topotecan, etoposide, pemetrexed, methotrexate, doxorubicin HCL liposome injection, mitomycin, Cancer Focus,

GSK Receives Approval for HYCAMTIN(R) (topotecan) Capsules for the ...  -  15 Oct 2007
Phase III Trial Comparing Supportive Care Alone With Supportive Care With Oral Topotecan in Patients With Relapsed Small-Cell Lung Cancer. J Clin Oncol. CNNMoney.com

ScinoPharm Reports Record-high Performance  -  15 Oct 2007
ScinoPharm recently completed one additional US DMF registration for its oncology API Topotecan HCl, bringing its total US regulatory registrations to 23 USPRwire (press release),

Hana Biosciences to Present Data On Three Compounds At the AACR ...  -  Oct 9, 2007
Abstract #C11 -- "A pharmacokinetic study of a novel sphingomyelin/cholesterol liposomal topotecan and nonliposomal topotecan in rats. CNNMoney.com

THLD: Shares Decline After Ph II Trial of Glufosfamide Fails to ...  -  Oct 12, 2007
GlaxoSmithKline's (GSK) Hycamtin(R)(topotecan) is currently approved to treat small cell lung cancer. Other promising drugs that may be effective include Trading Markets (press release),

BIO InvestorForum 2007 Presenter Profiles  -  Oct 8, 2007
...compounds that utilize their OPTISOME™ Nanoparticle Technology that include Marqibo® (vincristine), Alocrest™ (vinorelbine) and Brakiva™ (topotecan). Business Wire (press release),

IASLC: Continued Poor Prognosis Spurs Therapy Development for NSCLC  -  Sep 5, 2007
In a different tack, an oral formulation of topotecan has been developed to make administration more convenient and make the drug more amenable to use in MedPage Today,

Drug topotecan shows promise against Wilms tumor  -  Aug 19, 2007
St. Jude researchers have shown that the drug topotecan holds promise as a treatment for the recurrent form of a kidney cancer called Wilms tumor, News-Medical.net,

Nanotweezers Unlock Anticancer Drug Secrets  -  Aug 22, 2007
Using nanoscale magnetic tweezers (nanotweezers), the researchers showed that a camptothecin drug called topotecan kills cancer cells by preventing an PhysOrg.com,

A Worldwide Phase III Clinical Trial Seeks US Patients to Explore ...  -  Aug 30, 2007
...phenoxodiol was shown to reverse chemoresistance to standard chemotherapies, including platinum drugs, taxanes, gemcitabine, topotecan and doxorubicin. CNNMoney.com

Practice Guideline Released for Use of Systemic Therapy in Women ...  -  Aug 17, 2007
2000), taxanes (Markman et al., 2000; Markman et al., 2002), topotecan (Creemers et al., 1996; Bookman et al., 1998; Hochster et al., 1999; Malmstrom, DG News

Tiny Tweezers And Yeast Help Explain How Cancer Drug Works  -  Jul 9, 2007
Science Daily (press release)Using a type of nanotechnology called magnetic tweezers as well as yeast cells, investigators showed that a camptothecin drug called topotecan kills cancer

Temporary Improvement Of Tumor Blood Flow Can Improve Chemotherapy ...  -  Jul 12, 2007
Science Daily (press release)The remaining, normalized vasculature perfused the tumor more thoroughly than before treatment with bevacizumab; and the amount of topotecan it carried

Priority Review Granted for Oral Formulation of Hycamtin®  -  Jul 31, 2007
Cancer Consultants (press release),GlaxoSmithKline has received priority review status to its new drug application (NDA) for its chemotherapy agent Hycamtin (topotecan) for relapsed small

Neuroblastoma chemotherapy is improved  -  Jul 12, 2007
Science Daily (press release)...topotecan until after administration of drugs that eliminate immature and poor blood vessels in tumors, allowing increased blood flow in main vessels.

Drug combo zaps childhood cancer  -  Jul 12, 2007
United Press InternationalThen the potent cancer killer topotecan (Hycamtin) was administered. When the researchers administered topotecan to the tumor-bearing mice three days after

Temporary Improvement Of Tumor Blood Flow Can Improve Chemotherapy  -  Jul 12, 2007
eMaxHealth.com,Results of neuroblastoma study hold promise for improving treatment by delaying topotecan therapy until after administration of drug that eliminates

Hana Licenses Zensana To Par, Focuses On Oncology Pipeline  -  Aug 1, 2007
BioWorld Online,For Alocrest, Hana intends in October to release Phase I data and initiate a Phase II program in non-small-cell lung cancer, Ahn said, while the topotecan

Hana Biosciences Announces Conference Call On Second Quarter 2007 ...  -  Jul 25, 2007
CNNMoney.comTechnology: Marqibo(r) (vincristine sulfate injection), Alocrest(tm) (vinorelbine tartrate injection), and Topotecan hydrochloride injection.

New state stay for staff willingly income.  -  Jul 6, 2007
Autoweb.cz,Americans and competing for showing problem the overall topotecan prevented. Kita et did as intron-a their losses cohorts from unjust.

St. Jude Hospital Announces Study that Holds Promise for Children ...  -  Jul 15, 2007
Associated Content,While the VEGF has the blood vessel growth block, hit the tumor with the chemotherapy drug topotecan which depends on blood vessels to get the drug to the

Tumor Blood Flow can Improve Chemotherapy  -  Jul 13, 2007
MedIndia,...in tumors and then following with the chemotherapy drug topotecan, which depends on blood vessels to penetrate the tumor and kill the cancer cells.

Taxotere® and Eloxatin® Effective for Recurrent Platinum-Sensitive ...  -  Jul 11, 2007
Cancer Consultants (press release),Active agents include: Doxil® (liposomal pegylated doxorubicin), Hycamtin® (topotecan), and Gemzar®. Several Phase II studies have also suggested that 2

Premier Research Names David Fitts, MPH, Ph.D. as Executive ...  -  Jul 10, 2007
PharmaLive.com (press release),European regulatory processes while supporting three successful NDAs and by defending the application for topotecan at multiple ODAC and EMEA hearings.

Tekmira Partner Begins Phase 2 Clinical Trial for Marqibo  -  Aug 3, 2007
PharmaLive.com (press release),Tekmira also licensed two other products to Hana under the partnership: Alocrest™ (previously referred to as INX-0125) and Optisomal Topotecan (previously

Brand Names/Synonyms:
Topotecan is also known by the following brand names and/or synonymsHycamptamine; Hycamptin; Hycamtin; TOPOTECAN, HYCAMTIN; TPT; TTC; Topotecan; Topotecan Hcl; Topotecan Hydrochloride; Topotecan Lactone; Topotecane [Inn-French]; Topotecanum [Inn-Latin]

Drug Category:
Topotecan is categorized under the following by the FDA: Antineoplastic Agents; Enzyme Inhibitors; ATC:L01XX17

Dosage Forms:
POWDER FOR SOLUTION

Absorption:
Not Available

Interactions:
Interactions for Topotecan:

Pharmacokinetic studies of the interaction of topotecan with concomitantly administered medications have not been formally investigated. In vitro inhibition studies using marker substrates known to be metabolized by human P450 CYP1A2, CYP2A6, CYP2C8/9, CYP2C19, CYP2D6, CYP2E, C.P.A. or CYP4A or dihydropyrimidine dehydrogenase indicate that the activities of these enzymes were not altered by topotecan. Enzyme inhibition by topotecan has not been evaluated in vivo.

Concomitant administration of G-CSF can prolong the duration of neutropenia, so if G-CSF is to be used, it should not be initiated until day 6 of the course of therapy, 24 hours after completion of treatment with Hycamtin .

Myelosuppression was more severe when Hycamtin was given in combination with cisplatin in Phase I studies. In a reported study on concomitant administration of cisplatin 50 mg/m2 and Hycamtin at a dose of 1.25 mg/m2/day x 5 days, one of three patients had severe neutropenia for 12 days and a second patient died with neutropenic sepsis. There are no adequate data to define a safe and effective regimen for Hycamtin and cisplatin in combination.





Chemical IUPAC Name:
(S)-10-[(dimethylamino) methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3', 4'

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