Originally produced as potential chemical warfare agents during World War I and II, nitrogen mustard compounds, including Chlorambucil, were soon marketed as pharmaceuticals (CDC website, n
Data suggest accelerated metabolism and elimination of chlorambucil and phenylacetic acid mustard, but reduced oral bioavailability of chlorambucil cannot be excluded
1016/0006-2952(80)90489-x
Eleven male Sprague-Dawley rats (140-180g) were treated i
2003
McLean , D
The metabolic dispositionof chlorambucil, 4-p-(di-2-chloroethyl)aminophenylbutyric acid, was studied in the rat
Serum half-life is approximately 90 minutes with drug metabolism involving both methylation and beta-oxidation
Chlorambucil is used in the treatment of leukemias, some lymphomas, nephrosis, and inflammatory conditions such as sarcoidosis
It is not curative in any of these disorders but may produce clinically useful
Chlorambucil and its major metabolite undergo oxidative Chlorambucil is a slow-acting nitrogen mustard that alkylates and effectively cross links DNA, leading to altered protein production
Chlorambucil may increase the risk that you will develop other cancers
Examples of conditions the drug may be used for include lymphocytic leukemia, multiple myeloma, glomerulonephritis, non-erosive arthritis, immune-mediated skin disease, feline pemphigus foliaceous and severe feline eosinophilic granuloma complex
Chlorambucil and its major metabolite undergo oxidative In the present work we investigated the interaction of the chemotherapeutic drug chlorambucil (CBL) with human GSTA1-1 (hGSTA1-1) using kinetic analysis, protein crystallography and molecular dynamics
Hepatocellular carcinomas express the Na (+)-dependent bile acid transporter NTCP
We establish that chlorambucil is specifically toxic to BRCA1/2-deficient cells, including olaparib-resistant and cisplatin-resistant ones, suggesting the potential clinical use of chlorambucil against disease which has become resistant to these drugs
If the DNA is damaged by chlorambucil the cancer cells cannot grow
2 mg tablets
Those conjugates bearing two or four sterols show improved hydrolytic stability and water solubility relative to chlorambucil
Mitochondrial targeting of this agent dramatically potentiates its activity, and promotes apoptotic cell death in a variety of Chlorambucil is an orally administered alkylating agent which is currently used in the therapy of chronic lymphocytic leukemia, Hodgkin and non-Hodgkin lymphomas, and rarely in severe autoimmune conditions including rheumatoid arthritis, uveitis and nephrotic syndrome
In the rat prednimustine, the prednisolone ester of chlorambucil, is much less toxic than equimolar doses of chlorambucil, when administered subcutaneously (SC)
The mechanisms involved in the bioavailability of chlorambucil or 4-[p-(bis[2-hydroxyethyl]amino)phenyl]-butyric acid are poorly understood
Chlorambucil / metabolism* Chlorambucil / pharmacology Hydrogen-Ion Concentration Immunoglobulin G Lymphoma / immunology Lymphoma / metabolism Mice Mice, Inbred C57BL Chlorambucil / metabolism* Chromatography, High Pressure Liquid Ethacrynic Acid / pharmacology* Female Glutathione / metabolism* Glutathione Transferase / antagonists & inhibitors Glutathione Transferase / isolation & purification Antagonizes purine metabolism: 2 mg/kg PO q24h for 1-2 weeks, then 1-2 mg/kg q48h: GI upset, myelosuppression, acute pancreatitis, GI disorders, hepatotoxicity, infection, malignancy: Chlorambucil: Alkylating agent: 0
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Chlorambucil is taken orally (by mouth) in pill form
We administered orally 100mg (50 mg X 2/day of bestrabucil for 3 days), and dete
It should be given on an empty stomach 12 because giving it with food decreases bioavailability
The mean phenylacetic acid mustard plasma terminal phase half-life was approximately 1
This preliminary pharmacokinetic data suggests that oral chlorambucil Phenylacetic acid mustard (PAM; 2), a major metabolite of the anticancer agent chlorambucil (CLB; 1), was allowed to react with 2'-deoxyadenosine (dA), 2'-deoxyguanosine (dG), 2'-deoxycytidine (dC), 2'-deoxy-5-methylcytidine (dMeC), and thymidine (T) at physiological pH (cacodylic acid, 50% base)
Chlorambucil is rapidly absorbed following administration to animals as a solution or as an emulsion ( Newell et al
Originally produced as potential chemical warfare agents during World War I and II, nitrogen mustard
CAS number: 305-03-3
1016/j
1976 Oct 15;25(20):2331-5
Chlorambucil, approved by the Food and Drug Administration (FDA) in 1957, is an antineoplastic/alkylating agent with a broad spectrum of antitumor activity used to treat
The nitrogen mustard Chlorambucil (Chl) generates covalent adducts with double-helical DNA and inhibits cell proliferation
The metabolism of chlorambucil - ScienceDirect
Interactions
Call your doctor for medical advice about side effects
In vitro, chlorambucil is 99% bound to plasma proteins, specifically albumin
Weigh at least 2
A sensitive and specific method for the determination of chlorambucil and its metabolite in biological fluids is reported
However, the
Chlorambucil, gamma [rho-di(2-chloroethyl) aminophenyl] butyric acid, was labelled in either the carboxylic group (Ia), the mustard radical (Ib), or the carbon atom in the aplha position in the carboxylic group (Ic)
The metabolism of chlorambucil in vivo was investigated by examining tlie blood of drug- treated animals
Hepatocellular carcinomas express the Na (+)-dependent bile acid transporter NTCP
This is a purine analog considered to be the most efficacious agent for the treatment of chronic lymphocytic leukemia
It controls everything the cell does
Physical properties
Below is a text only representation of the Patient Information Leaflet (ePIL)
Those conjugates bearing two or four sterols show improved hydrolytic stability and water solubility relative to chlorambucil
Here, we report, to our knowledge, the first successful delivery of an active DNA alkylating agent--chlorambucil--to mitochondria, and describe unexpected features that result from rerouting this drug within the cell
1016/s0305-7372(79)80005-5
The effects of different matrices on the disintegration of chlorambucil were investigated by HPLC, 1H NMR, 31P NMR, and mass spectrometry