Fludarabine Phosphate

Fludarabine Phosphate is the preferred second-line therapy for chronic lymphocytic leukaemia once initial alkylating agent therapy fails, and may also be used for initial therapy. Fludarabine Phosphate belongs to the antimetabolite class of antineoplastics. Fludarabine Phosphate is structurally similar to vidarabine (an antiviral agent) and cytarabine.It has also been tried in other malignancies. fludarabine phosphate is used for the treatment of chronic lymphocytic leukaemia. Fludarabine Phosphate is potentially active against a variety of other malignancies, including indolent low-grade non-Hodgkin's lymphoma, mycosis fungoides, heavy chain disease, prolymphocytic leukaemia, hairy cell leukaemia, and Waldenström's macroglobulinaemia.

Fludarabine Phosphate’s innovator is Bayer-Global and is known world-wide be the brand name Fludara.

Fludarabine Phosphate acts as a cytotoxic purine antimetabolite. Upon administration, Fludarabine Phosphate is rapidly dephosphorylated in the plasma to free nucleoside 9-beta-D-arabinosyl-2 fluoroadenine (F-ara-A), which then enters into the cell via high and low affinity transport systems. The rate of transport of Fludarabine Phosphate into malignant cells is greater than that into normal cells. Intracellularly, F-ara-A is converted to the 5'-triphosphate, F-ara-ATP. The rate limiting step in this process is the formation of the monophosphate, which is catalyzed by deoxycytidine kinase. Cells that lack deoxycytidine kinase are resistant to Fludarabine Phosphate. The cytotoxicity of F-ara-ATP is primarily due to its effects on DNA. F-ara-ATP competes with deoxyadenosine triphosphate for incorporation into DNA. Once incorporated into DNA, F-ara-ATP functions as a DNA chain terminator, preventing the elongation of DNA strands at the Fludarabine Phosphate'-terminal. F-ara-ATP also inhibits DNA repair by specifically inhibiting DNA polymerase alpha, gamma, and delta.

In addition, F-ara-ATP decreases deoxynucleotide pools by inhibiting ribonucleoside diphosphate reductase. By decreasing deoxynucleotide pools, Fludarabine Phosphate enhances the activity of deoxycytidine kinase, the enzyme required for phosphorylation of F-ara-A. F-ara-A also inhibits DNA primase and DNA ligase I resulting in DNA deletions and mutations. Incorporation into RNA and inhibition of RNA transcription occurs leading to decreased mRNA and protein production, and may be relevant to the activity of Fludarabine Phosphate in indolent diseases. However, 10-fold higher intracellular concentrations are required to inhibit DNA versus RNA. Fludarabine Phosphate depletes CD4+ cells leading to immunosuppression. Combination chemotherapy regimens have been designed to enhance the cytotoxicity of Fludarabine Phosphate by enhancing the accumulation of the triphosphate form or by combining Fludarabine Phosphate with DNA damaging agents that inhibit DNA repair mechanisms.

Fludarabine Phosphate appears in the following formulation and dosage:
Intravenous Powder for Sollution: 50 mg
Tablets: 10 mg

General data on Fludarabine Phosphate Active Pharmaceutical Ingredient

CAS Registry: 75607-67-9
ATC: L01BB05
Molecular Formula: C10H1+FN5O7P
Molecular Weight: 365.2
Pharmacopoeias: In Eur. and US.

Ph. Eur. 5.5: Fludarabine Phosphate is a white or almost white, hygroscopic, crystalline powder. Fludarabine Phosphate is slightly soluble in water; very slightly soluble in dehydrated alcohol; freely soluble in dimethylformamide.

USP 30: Fludarabine Phosphate is a white to off-white, hygroscopic, crystalline powder. Fludarabine Phosphate is slightly soluble in water and in 0.1M hydrochloric acid; practically insoluble in dehydrated alcohol; freely soluble in dimethylformamide.

TAPI's Fludarabine Phosphate Pharmaceutical Ingredient

TAPI's Fludarabine Phosphate Active Pharmaceutical Ingredient is produced in Sicor- Società Italiana Corticosteroidi S.r.l Rho site in Milano, Italy.

Fludarabine Phosphate is a highly potent active pharmaceutical ingredient. Fludarabine Phosphate belongs to the hormone contraceptive and replacement therapy group of drugs. These drugs are highly potent active pharmaceutical ingredients that need special handle in production or preparation. As a highly potent drug, Fludarabine Phosphate is considered to be small volume Active Pharmaceutical Ingredient.

TAPI provides full service on Fludarabine Phosphate and other APIs in our portfolio. We provide information on TAPI's Fludarabine Phosphate, the regulatory compliance with various health regulations and documentation. Contact us today for further inquiries and samples and kilograms availability information for TAPI's Fludarabine Phosphate.

TAPI is a world leading developer and manufacturer of highly potent drugs used by innovative and generic companies to formulate their final dosage medications. TAPI highly potent manufacturing plants are located mainly in Italy (Sicor S.r.l. ) and Mexico (Sicor de Mexico) . TAPI highly potent active pharmaceutical ingredients, such as Fludarabine Phosphate, are used in oral, parenteral, topical and inhalation therapies; and most fall in four classes: Steroids, Oncolytics, Hormones, Non-depolarizing muscle relaxants, Immunosuppressants.

2008 Available DMF: U.S. DMF, EU CTD, CEP and Russia DMF.

Other products, in the group of ANTINEOPLASTIC AGENTS - Miscellaneous antineoplastics available on TAPI's portfolio are:  Bicalutamide,Bortezomib,Etoposide,Fluorouracil and Pemetrexed Diacid.

Contact us today for information on TAPI's Fludarabine Phosphate  and other highly potent Active Pharmaceutical Ingredients.

Legal Note

Product exploitation, including development, sales and offer for sale are performed where permissible by patent law. This presentation is not and should not constitute an offer for sale in territories where it is not permitted by law. In USA Products  that  Currently on Patent are available for R&D Use in Accordance with 35 USC §271 (e) (1).

*TAPI stands for Teva's Active Pharmaceutical Ingredients