Cladribine

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


Overview:

Cladribine
(when available)

Pharmacology and use:
Cladribine is a synthetic antineoplastic agent indicated for the treatment of active Hairy Cell Leukemia as defined by clinically significant anemia, neutropenia, thrombocytopenia or disease-related symptoms. Cladribine is an antimetabolite. Cladribine's action is cell cycle-phase nonspecific; cladribine affects both dividing and resting lymphocytes. For the treatment of active Hairy Cell Leukemia as defined by clinically significant anemia, neutropenia, thrombocytopenia or disease-related symptoms

Mechanism Of Action:
Cladribine is structurally related to fludarabine and pentostatin but has a different mechanism of action. It is phosphorylated by deoxycytidine kinase to the corresponding nucleotide CdATP which accumulates and is incorporated into the DNA of cells such as lymphocytes. The phosphorylated metabolites of cladribine tend to accumulate in cells with a high ratio of deoxycytidine kinase activity to 5' nucleotidase activity (lymphocytes, monocytes ) and are converted to the active triphosphate deoxynucleotide. Intracellular accumulation of toxic deoxynucleotides selectively kills these cells, which become unable to properly repair single-strand DNA breaks, leading to disruption of cell metabolism. In addition, there is some evidence that deoxynucleotides are incorporated into the DNA of dividing cells and impair DNA synthesis. Cladribine also induces apoptosis (a form of programmed cell death in sensitive cells). Cladribine is resistant to the action of adenosine deaminase (ADA), which normally deaminates deoxyadenosine to deoxyinosine.

News Articles on Cladribine

MS Market is Estimated to Be Worth Almost US$8 Billion in 2008 ...  -  Sep 2, 2008
These include: Novartis' fingolimod, Teva's laquinimod, Merck KGaA's Mylinax (cladribine), sanofi-aventis' teriflunomide and Biogen Idec's BG-12 in Phase MarketWatch

The Multidisciplinary Team in Multiple Sclerosis: Harnessing the ...  -  Aug 18, 2008
Discussion of Off-Label, Investigational, or Experimental Drug Use: Cladribine, fingolimod, and teriflunamide. Disclosure: Dr. Turner: Sources of Funding Medscape (subscription)

Cladribine Achieves High Response Rates in Mantle Cell Lymphoma  -  Aug 1, 2008
By Martha Kerr NEW YORK JUL 31, 2008 (Reuters Health) - The purine nucleoside analogue cladribine (2-CDA) achieves high response rates and significantly Cancerpage.com,

Bipolar and Chemotherapy  -  Jun 12, 2008
In June 2006, I underwent a five-day out-patient treatment regimen with Cladribine, 2-chlorodeoxyadenosine (2Cda). Within a week of that treatment, HealthCentral.com,

Multiple Sclerosis Treatment: The Fundamentals  -  Jun 28, 2008
Most of the research you read about is aimed at disease modification: the oral medications (Cladribine, Fingolimod, Teriflunomide, BG00012, Laquinomod, etc. HealthCentral.com,

Merck Serono's Rebif(R) Celebrates 10th Anniversary  -  Jun 9, 2008
The most advanced projects are cladribine tablets, currently in Phase III, and atacicept, currently in Phase II. With regulatory filing expected in 2009, PR Newswire UK (press release),

Merck Serono and Bionomics Announce Multiple Sclerosis Development ...  -  Jun 18, 2008
Additional therapeutic options are currently under development at Merck Serono, including oral cladribine, currently in Phase III and potentially the first PR Newswire UK (press release),

Results Of A Phase 3 Study Show TORISEL Significantly Improved ...  -  Jun 9, 2008
...or investigators' choice of one of the following single agents at predefined doses: gemcitabine, fludarabine, chlorambucil, cladribine, etoposide, Medical News Today (press release),

High-Dose Temsirolimus Superior to Investigator's Choice Regimens ...  -  Jun 6, 2008
The most common investigator-assigned drugs were gemcitabine (42%) and fludarabine (26%), followed by chlorambucil, vinblastine, alemtuzumab, cladribine, DG News

Oral Drug From Novartis/Mitsubishi Tanabe Will Capture The  -  May 30, 2008
The report also finds that other strong contenders in the multiple sclerosis market over the next 10 years will include Merck Serono's oral cladribine Pharmaceutical Online (press release),

New Data Show TORISEL Improves Progression-Free Survival for ...  -  May 31, 2008
...or investigators' choice of one of the following single agents at predefined doses: gemcitabine, fludarabine, chlorambucil, cladribine, etoposide, FOXBusiness

Merck Serono Launches New Formulation Of Interferon Beta-1a  -  Mar 3, 2008
Additional therapeutic options are currently under development at Merck Serono, including cladribine, currently in Phase III, as well as several products in Medical News Today (press release),

Risk for Second Nonlymphoid Neoplasms in Chronic Lymphocytic Leukemia  -  Nov 16, 2007
Second malignancies and Richter's syndrome in patients with chronic lymphocytic leukaemia treated with cladribine. Eur J Cancer. 2004;40:383-389. Medscape (subscription)

ã€?页é?¢è°ƒè‰²ç‰ˆ  -  Nov 14, 2007
...inhibitors of DNA synthesis/repair (teriflunomide; Sanofi-Aventis, cladribine; Ivax/Serono), potassium channel blockers (fampridine; Acorda, BNC-245; 金�界,

Teva starts Phase III trials of oral drug laquinimod for MS  -  Nov 8, 2007
Other companies developing oral drugs for MS in late-stage trials include Novartis with FTY720 (fiungolimod) and Merck Serono with Mylinax (cladribine), Pharma Times (subscription),

Two-year Phase IIIb data show that the new formulation of Rebif ...  -  Oct 12, 2007
Additional therapeutic options are currently under development at Merck Serono, including oral cladribine, currently in Phase III and potentially the first PipelineReview.com (press release),

Interferon Beta-1a Offers A Near 3-fold Improvement In Injection ...  -  Oct 11, 2007
Additional therapeutic options are currently under development at Merck Serono, including cladribine, currently in Phase III, as well as several products in Medical News Today (press release),

EU approval of new Rebif just what the doctor ordered  -  Aug 30, 2007
Merck is indeed just one of the companies racing to create an oral treatment and currently has its oral cladribine formulation in Phase III trials, BiopharmaReporter.com,

New Formulation of Multiple Sclerosis Treatment Rebif(R) Approved ...  -  Aug 29, 2007
Additional therapeutic options are currently under development at Merck Serono, including oral cladribine, currently in Phase III and potentially the first ITNews,

Early signs death with viruses range marry.  -  Jul 9, 2007
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Drug Discovery Research: New Frontiers in the Post-Genomic Era  -  Jun 29, 2007
PharmaLive.com (press release),2-CHLORODEOXYADENOSINE (CLADRIBINE): RATIONAL DEVELOPMENT OFA NOVEL CHEMOTHERAPEUTIC AGENT (Howard B. Cottam and Dennis A. Carson,* Moores Cancer Center,

Reformulated Rebif right on track  -  Jun 28, 2007
BiopharmaReporter.com,The company earlier this year announced that it had completed enrolment in its Phase III trials for Movectro, its proprietary oral formulation of cladribine

Costs Increase for Multiple Sclerosis Therapies, Tiering, Usage ...  -  Jun 12, 2007
Atlantic Information Services, Inc.,Among those anticipated oral therapies are IVAX Corp. and Serono's Mylinax (cladribine), Novartis' Fingolimod (FTY720), sanofi-aventis' Teriflunomide (HMR

Extended storage for Teva MS drug  -  Jun 6, 2007
In-PharmaTechnologist.com,The company is also in the process of developing an oral MS treatment based on cladribine which could prove particularly lucrative if it can win the race to

Merck Serono Completes Patient Enrollment in CLARITY Phase III ...  -  Jan 16, 2007
Drug Newswire (press release),..."The completion of patient enrollment into the CLARITY pivotal trial is a major milestone in the development program of oral cladribine," said Franck

Sección internacional  -  Jan 15, 2007
Bolsamania.com,...(PRN) - Merck Serono Completes Patient Enrollment in CLARITY Phase III Pivotal Clinical Trial of Oral Cladribine ... [+]

Biotech Stocks Day-in-Review: BioCryst Begins Pivotal Trial of ...  -  Jan 17, 2007
Seeking Alpha,Merck Serono [SRA] has completed enrollment in a Phase III trial of an oral formulation of cladribine for relapsing forms of multiple sclerosis.

Sección internacional  -  Jan 16, 2007
Bolsamania.com,...(PRN) - Merck Serono Completes Patient Enrollment in CLARITY Phase III Pivotal Clinical Trial of Oral Cladribine ... [+]

Sección internacional  -  Jan 16, 2007
Bolsamania.com,...(PRN) - Merck Serono Completes Patient Enrollment in CLARITY Phase III Pivotal Clinical Trial of Oral Cladribine ... [+]

(PRN) - Following Is a Test Release ... [+]  -  Jan 15, 2007
Bolsamania.com,...(PRN) - Merck Serono Completes Patient Enrollment in CLARITY Phase III Pivotal Clinical Trial of Oral Cladribine ... [+]

Clinical Trial Design  -  Nov 27, 2006
Medscape (subscription)Oral cladribine is currently being investigated in a phase 3, multicenter international trial for MS. Although the results of this trial are pending,

Serono Announces Initiation of the Reflex Trial to Evaluate New ...  -  Dec 12, 2006
Drug Newswire (press release),Additional therapeutic options are currently under development at Serono, including oral cladribine, currently in Phase III studies and potentially the

2006 - A Very Good Year in MS Research  -  Dec 7, 2006
PR Newswire (press release),...a large phase III trial is now underway; -- oral cladribine (an immune-modulating drug by Serono), now being tested in an international Phase 3 clinical

Scientists improve cancer drug synthesis  Nov 2, 2006
02/11/2006 - Researchers have developed a more efficient and cost-saving method to make cladribine, a drug used for the treatment of certain types of leukaemia ... -In-PharmaTechnologist.com, US FDA gives fast track status to Serono's oral cladribine for ...  Oct 12, 2006
Serono (SEO) announced that oral cladribine has been designated a fast track product by the US Food and Drug Administration (FDA). ... -Therapeutics Daily (subscription) (press release), BYU scientists offer a new way to manufacture cancer drug  Oct 30, 2006
...of cancer. The new manufacturing method is considered a more efficient way to synthesize the drug known as cladribine. The findings ... -Salt Lake Tribune, Serono Q3 Adj. Profit Rises 15.5% On Strong Sales Of Rebif And ...  Oct 19, 2006
In September 2006, oral drug, cladribine was designated a Fast Track product for patients with relapsing forms of multiple sclerosis by the US Food and Drug ... -Trading Markets, Serono Delivers Strong Adjusted* Net Income of $183.5m in Third ...  Oct 18, 2006
...in several R&D programs: - In-licensing of safinamide in early Phase 3 in Parkinson's Disease - Fast Track designation for oral cladribine in relapsing forms ... -PR Newswire (press release), Serono posts better-than-forecast Q3 results, driven by MS drug ...  Oct 19, 2006
Cladribine treatment Novantrone sales in the third quarter were 2.8 mln usd, down 84.6 pct hit by the introduction of generics in the US in April 2006. ... -Forbes, Pharma Earnings On Tap-Upcoming Week In Earnings  Oct 17, 2006
In late September, Serono said it received a Fast Track product designation from the FDA for its purine nucleoside analogue, cladribine. ... -Trading Markets, European Commission Approves Revision of Therapeutic Indication ...  Jul 9, 2006
Additional therapy options are currently under development at Serono, including cladribine tablets, currently in Phase III studies and potentially the first ... -Yahoo! News



Phase III Trial Of Oral Cladribine, A Novel Investigational ...  May 5, 2006
Serono (drt-x: SEO and NYSE: SRA) announced today that recruitment in the US is beginning for the Phase III CLARITY study (CLAdRIbine Tablets in Treating MS ... - Medical News Today

Phase III Trial of Oral Cladribine, a Novel Investigational ...  May 4, 2006
May 4, 2006 /PRNewswire-FirstCall/ -- Serono announced today that recruitment in the US is beginning for the Phase III CLARITY study (CLAdRIbine Tablets in ... - PharmaLive.com

Serono's Oral Drug Enrollment Is Challenging  May 5, 2006
0606 GMT [Dow Jones] Serono's (SRA) enrollment for the last phase of clinical testing of its oral multiple sclerosis drug Cladribine could be challenging ... - newratings.com

Serono expands multiple sclerosis trial to US  May 5, 2006
Serono has begun enrolling patients in the US into a phase III trial of oral cladribine for the treatment of patients with relapsing forms of multiple sclerosis ... - Pharmaceutical Business Review

Serono Enrolling US Patients To Oral MS Drug Trial -2-  May 4, 2006
MS drug to the market. Oral cladribine is also known under its suggested brand name Mylinax. Current treatments typically belong ... - Therapeutics Daily (subscription)





Teva Ends Work on Oral Copaxone  Mar 21, 2006
The Ivax-Serono product, called Mylinax, is a pill version of injectable cladribine, which treats a form of leukemia. "Previous ... - TheStreet.com

Tysabri poised for return to market  Mar 31, 2006
...mitoxantrone hydrochloride) and Serono/Pfizer's Rebif (r-IFN-B1a) loom as Tysabri's main competitors, while Serono's Mylinax (cladribine) (expected to file for ... - Pharmaceutical Business Review

Biogen says Tysabri, new pill to keep it MS leader  Mar 10, 2006
...currently conducting Phase III tests on its FTY720 drug to be used as an oral treatment for MS, while Serono also has an oral version of its cladribine drug in ... - Reuters

Serono's 2005 Adjusted(i) EPS Increased by 34.6% Feb 5, 2006
...m - Progress in key MS clinical trials - REGARD 1st year of treatment completed in Rebif(R) vs Copaxone head-to-head study - CLARITY: oral cladribine Phase III ... - PR Newswire,

Seronons 2005 Adjusted(i) EPS Increased by 34.6%  Feb 5, 2006
...of treatment. The Phase III CLARITY (CLAdRIbine Tablets Treating MS OrallY) study of oral cladribine is enrolling patients. In 2005 ... - MSN Money

Serono sales, profits miss forecasts, mum on M&A Feb 5, 2006
Serono also said it had started enrolling patients to take part in a Phase III trial for its oral cladribine drug, one of the two frontrunners in the race to ... - Reuters

Serono: On the Block and On the Clock  Feb 9, 2006
An oral drug for MS (cladribine) has a long and not-so-illustrious history, and I'm similarly not too optimistic on other drugs like zanolimumab (cancer) or ... - Motley Fool

Serono sales, profits miss forecasts, mum on M&A Feb 6, 2006
Serono also said it had started enrolling patients to take part in a Phase III trial for its oral MS drug cladribine and said it was confident it would beat ... - Reuters

Serono: On the Block and On the Clock  09 Feb 2006
An oral drug for MS (cladribine) has a long and not-so-illustrious history, and I'm similarly not too optimistic on other drugs like zanolimumab (cancer) or ... - Motley Fool

Serono's 2005 Adjusted(i) EPS Increased by 34.6%  Feb 5, 2006
...m - Progress in key MS clinical trials - REGARD 1st year of treatment completed in Rebif(R) vs Copaxone head-to-head study - CLARITY: oral cladribine Phase III ... - PR Newswire

Seronons 2005 Adjusted(i) EPS Increased by 34.6%  Feb 5, 2006
...of treatment. The Phase III CLARITY (CLAdRIbine Tablets Treating MS OrallY) study of oral cladribine is enrolling patients. In 2005 ... - MSN Money

Serono sales, profits miss forecasts, mum on M&A  Feb 5, 2006
Serono also said it had started enrolling patients to take part in a Phase III trial for its oral cladribine drug, one of the two frontrunners in the race to ... - Reuters

Serono sales, profits miss forecasts, mum on M&A  Feb 6, 2006
Serono also said it had started enrolling patients to take part in a Phase III trial for its oral MS drug cladribine and said it was confident it would beat ... - Reuters

Brand Names/Synonyms:
Cladribine is also known by the following brand names and/or synonyms2 Chlorodeoxyadenosine; Chlorodeoxyadenosine; Cladribine; Cladribine [Usan:Ban:Inn]; Leustatin

Drug Category:
Cladribine is categorized under the following by the FDA: Immunosuppressive Agents; Antineoplastic Agents; ATC:L01BB04

Dosage Forms:
SOLUTION

Absorption:
Oral bioavailability is 34-48%

Interactions:
Interactions for Cladribine:

There are no known drug interactions with LEUSTATIN Injection. Caution should be exercised if LEUSTATIN Injection is administered before, after, or in conjunction with other drugs known to cause immunosuppression or myelosuppression.





Chemical IUPAC Name:
5-(6-amino-2-chloro-purin-9-yl)-2-(hydroxymethyl)oxolan-3-ol

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