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PubMed2005

Imatinib mesylate in chronic myeloid leukemia: a prospective, single arm, non-randomized study.

Chronic myeloid leukemia (CML) is a hematopoietic stem cell disorder characterized by the balanced reciprocal translocation t (9:22). The resulting fusion gene, the BCR-ABL, is responsible for oncogenesis. Imatinib mesylate is a novel molecule, which inhibits the protein product of this fusion gene and hence has been used in the treatment of CML. The present study evaluates 174 patients with CML treated with imatinib mesylate. Of these 174 patients, 97 were in chronic phase, 47 in accelerated phase and 30 patients had blast crisis. Patients in chronic phase received imatinib mesylate in the dose of 400-mg daily, while those in accelerated phase and blast crisis received 600 to 800 mg daily. Of the 97 patients with chronic phase, 49 patients (50.5%) achieved a major (major + complete) cytogenetic response. Of the 47 patients in accelerated phase, 10 patients (21.3%) achieved a major cytogenetic response and in 30 patients with blast crisis, 7 (23.3%) achieved a major cytogenetic response. Dermatitis, mucositis, neutropenia and thrombocytopenia were some of the major toxicities. Of interest, 121 of the 174 patients (69.5%) developed generalized hypopigmentation. We conclude that imatinib mesylate is a safe and effective first-line therapy for chronic myeloid leukemia.

Adolescent↗
PubMedDate not supplied

Very early detection of response to imatinib mesylate therapy of gastrointestinal stromal tumours using 18fluoro-deoxyglucose-positron emission tomography.

AIM: To investigate whether 18F-FDG-PET allows early assessment of response to imatinib mesylate in GIST patients. PATIENTS AND METHODS: Five gastrointestinal stromal tumour (GIST) patients and one patient with a KIT-positive small cell cancer were studied. Treatment consisted of 400 mg imatinib mesylate daily. 18F-deoxyglucose-positron emission tomography (18F-FDG-PET) scans were done before and one week after starting imatinib mesylate therapy. RESULTS: Metabolic responses were detected after only one week of therapy in all GIST patients (four partial and one complete response). The mean decrease of the standardised uptake value was 60% (range 43 to 77%). In contrast, the tumour of the non-GIST patient was metabolically stable. Four of the 5 GIST patients achieved a partial response on CT after a mean duration of 23 weeks (range 6 to 48 weeks). CONCLUSION: 18F-FDG-PET is a valuable method for the detection of response to imatinib mesylate in patients with KIT-positive tumours as early as one week after starting therapy.

Adult↗
PubMed2005

[Intestinal bleeding during the treatment of chronic myeloid leukemia with imatinib mesylate].

A 35-year-old woman attended our hospital with chronic myeloid leukemia and was prescribed imatinib mesylate. She was admitted with lower abdominal pain, stomatitis, and hyposthenia after an increase in her dose of imatinib mesylate. When the treatment was changed to interferon-alpha and Ara-C, the lower abdominal pain, stomatitis, and hyposthenia improved, but bone marrow aspiration showed 36.4% blasts. After the treatment was changed back to an increased dose of imatinib mesylate (800 mg), the stomatitis deteriorated and intestinal bleeding reoccurred. Endoscopy demonstrated the presence of multiple ulcers in the ascending colon and 99mTc RBC scintigraphy demonstrated lesions of the large and small intestine. The patient declined any treatment except for transfusion and died suddenly after ten days. The present case suggests that we should carefully consider the possibility of intestinal bleeding when prescribing imatinib mesylate.

Adult↗
PubMed2003

Fenoldopam mesylate for the prevention of contrast-induced nephropathy: a randomized controlled trial.

CONTEXT: The development of contrast-induced nephropathy in patients undergoing invasive cardiac procedures is associated with a marked increase in cardiovascular morbidity and mortality. Fenoldopam mesylate, a specific agonist of the dopamine-1 receptor, preserves renal blood flow after iodinated contrast administration and has shown promise in ameliorating contrast nephropathy in previous observational and small randomized trials. OBJECTIVE: To examine the efficacy of fenoldopam mesylate in preventing contrast nephropathy after invasive cardiovascular procedures. DESIGN: Prospective, placebo-controlled, double-blind, multicenter randomized trial with serial serum creatinine levels measured at a central biochemistry laboratory (at baseline and 1, 24, 48, and 72 to 96 hours after study drug administration) and 30-day clinical follow-up. PATIENTS AND SETTING: Between March 2001 and July 2002, 315 patients with creatinine clearance less than 60 mL/min (1.00 mL/s) at 28 centers in the United States were randomized to receive fenoldopam mesylate (n = 157) or placebo (n = 158). INTERVENTIONS: Patients were hydrated and randomized to receive intravenous fenoldopam (0.05 microg/kg/min titrated to 0.10 microg/kg/min) vs matching placebo, starting 1 hour prior to angiography and continuing for 12 hours. MAIN OUTCOME MEASURE: Contrast-induced nephropathy, defined as an increase of 25% or more in serum creatinine level within 96 hours postprocedure. RESULTS: Mean (SD) patient age was 70 (11) years, and 49% had diabetes mellitus. Mean (SD) baseline creatinine clearance was 29.0 (10.0) mL/min (0.48 [0.16] mL/s) (range, 7.5-56.8 mL/min [0.12-0.94 mL/s]), and 157 (108) mL of contrast was administered during the procedures. The primary end point of contrast-induced nephropathy occurred in 33.6% of patients assigned to receive fenoldopam vs 30.1% assigned to receive placebo (relative risk, 1.11; 95% confidence interval, 0.79-1.57; P =.61). There were no significant differences in the 30-day rates of death (2.0% vs 3.8%, P =.50), dialysis (2.6% vs 1.9%, P =.72), or rehospitalization (17.6% vs 19.9%, P =.66) in fenoldopam vs placebo randomized patients, respectively. CONCLUSION: The selective dopamine-1 agonist fenoldopam mesylate does not prevent further renal function deterioration after contrast administration in patients with chronic renal insufficiency.

Adult↗
PubMed1993

Fenoldopam mesylate versus sodium nitroprusside in the acute management of severe systemic hypertension.

Thirty-three patients with severe systemic hypertension defined as a diastolic blood pressure (DBP) > or = 120 mm Hg were randomized in a single-blind fashion to be treated with either intravenous fenoldopam mesylate (FNP) or sodium nitroprusside (NTP). Fenoldopam mesylate and NTP infusion rates began at 0.1 microgram/kg/minute and 0.5 microgram/kg/minute, respectively and were titrated to achieve a goal DBP of between 95 and 110 mm Hg; or a reduction of at least 40 mm Hg if the baseline DBP was > 150 mm Hg. Fenoldopam mesylate (n = 15) reduced blood pressure from 217/145 +/- 6/5 to 187/112 +/- 6/3 mm Hg (P < .001) at an average infusion rate of 0.5 +/- 0.1 microgram/kg/minute. The average time to achieve goal DBP with FNP was 1.5 +/- 1.4 hours. Nitroprusside (n = 18) reduced blood pressure from 210/136 +/- 5/2 to 172/103 +/- 6/2 mm Hg (P < .001) at an average infusion rate of 1.2 +/- .24 micrograms/kg/minute. Nitroprusside response time averaged 2 +/- 2.5 hours. There was no significant difference between the magnitude of effect seen with either FNP or NTP; nor was there any difference observed in the adverse effect rates of the two agents. Fenoldopam mesylate and NTP demonstrate similar overall efficacy in the treatment of severe systemic hypertension.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed1986

Gabexate mesylate inhibition of serine proteases: thermodynamic and computer-graphics analysis.

The inhibitory effect of gabexate mesylate, which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation, and as a regional anticoagulant agent for hemodialysis, has been measured on bovine factor Xa, bovine alpha-thrombin, human Lys77-plasmin, human urinary kallikrein, human urokinase, porcine pancreatic beta-kallikrein-B, and bovine beta-trypsin catalyzed hydrolysis of p-nitrophenyl esters of N-alpha-carbobenzoxy-L-arginine and N-alpha-carbobenzoxy-L-lysine. On the basis of enzyme:gabexate mesylate affinities, the serine proteases can be arranged as follows: human urinary kallikrein approximately porcine pancreatic beta-kallikrein-B much less than bovine beta-trypsin approximately bovine factor Xa approximately human Lys77-plasmin approximately human urokinase approximately bovine alpha-thrombin. The mode of binding of gabexate mesylate to the serine proteases conforms to the active-reactive site geometries observed in their complexes with natural and synthetic inhibitors. Differences in gabexate mesylate affinities for these proteases reflect structural differences at their primary specificity subsite, which have been investigated by comparative analysis of amino acid sequences and by computer-graphics techniques.

Animals↗
PubMed1994

Phase II evaluation of the AMAP, 773U82 mesylate, in pancreatic cancer.

Pancreatic cancer is the fifth leading cause in cancer related death among adults in the United States. Thirty-thousand new cases of pancreatic cancer are diagnosed each year, most are metastatic at diagnosis and no effective systemic therapy is available. 773U82 mesylate is one of a series of compounds (arylmethylaminopropanediols-AMAPS) which was synthesized at the Wellcome Research Laboratories. AMAPS bind to DNA, show evidence of topoisomerase 2 inhibition and are active in a variety of murine and human preclinical screens. Based on these data a phase II trial of 773U82 mesylate administered at 800 mg/m2 daily x 3 at a 4 h infusion repeated every three weeks was carried out. Patients eligible for these trials had histologic proof of adenocarcinoma, good performance status, and normal organ function. This was a multi-institutional trial. Nineteen patients were entered; 15 patients were fully eligible and 4 were ineligible, but were evaluated. Thirteen patients were fully evaluable for response and no response was seen. Median time to progressive disease among eligible patients was 56 days. Toxicity of 773U82 mesylate was myelosuppression which was not prohibitive. 773U82 mesylate is not active in pancreatic cancer.

Adenocarcinoma↗
PubMed1990

Assessment of hemodynamic tolerance from a 24-hour intravenous infusion of fenoldopam mesylate in congestive heart failure.

To determine the maintenance of pharmacodynamic effects of fenoldopam mesylate, a dopamine-1 agonist, the invasive hemodynamic profiles of 33 patients with New York Heart Association functional class III to IV congestive heart failure were examined. Fenoldopam mesylate was initiated at 0.1 micrograms/kg/min and titrated to a cardiac index greater than or equal to 25% above baseline. Upon achievement of optimal hemodynamics, maintenance infusion was begun (mean dose 0.6 micrograms/kg/min). Fenoldopam mesylate (baseline vs maximal effect) decreased systemic vascular resistance by 37% (p less than 0.001), left ventricular filling pressure by 16% (p less than 0.05) and mean arterial pressure by 11% (p less than 0.05), with an associated augmentation in cardiac index and stroke volume index by 27% (p less than 0.001). Attenuation of hemodynamic effect (maximal effect vs time) was noted in cardiac index (14% p less than 0.001), systemic vascular resistance (13% p less than 0.05) and stroke volume index (13% p less than 0.05). None of the parameters exhibited complete attenuation to baseline values. Fenoldopam mesylate improves cardiac output and lowers systemic vascular resistance with relative attenuation of pharmacodynamic effect during a 24-hour intravenous infusion.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed1986

Comparison of bronchodilator responses with bitolterol mesylate solution with the use of two different nebulizer systems in asthma.

Bitolterol mesylate is a beta 2-adrenergic bronchodilator that has been studied in a metered-dose inhaler formulation and as an aerosol in a closed, intermittent-flow nebulizer system. The optimum dose was found to be 1.0 mg in the closed system. In this dose-response study, 1.0 mg by closed-system nebulizer was compared with different doses delivered by an open, continuous-flow nebulizer system. Treatment with 2.5 mg of bitolterol mesylate in the open system is comparable to 1.0 mg in a closed system. Onset of bronchodilator activity occurred within 5 minutes for most patients, and median duration of action with different doses was 8 hours or longer. Mean maximum percent increases in FEV1 with 2.5, 3.5, and 4.5 mg of bitolterol mesylate with the open system were approximately 50% and comparable with that obtained with 1.0 mg with the closed system. Treatments with doses up to 3.5 mg in the open system were well tolerated with few side effects. We conclude that bitolterol mesylate is an effective, long-lasting bronchodilator when it is used as a nebulized aerosol by both open and closed delivery systems; a larger dose is optimal for the former system than for the latter. We believe that manufacturers' recommended doses should take into account the different efficiencies of open and closed nebulizer systems.

Adolescent↗
PubMed1986

Bitolterol mesylate in exercise-induced asthma.

Exercise-induced asthma is a useful model for evaluating the activity and duration of action of pharmacologic agents of asthma. The main objective of this double-blind, crossover study was to determine the effect of the aerosolized beta-adrenergic agent, bitolterol mesylate, on exercise-induced asthma while its efficacy was being compared with isoproterenol and placebo. Twelve subjects with exercise-induced asthma performed cycloergometer exercise 45 minutes after three inhalations of bitolterol mesylate aerosol (1050 micrograms), or isoproterenol (255 micrograms), or placebo in random sequence. Bitolterol mesylate aerosol was very effective in protecting against exercise-induced asthma. The mean percent maximal decrease of FEV1 after exercise was 5.0% for bitolterol, 22.2% for isoproterenol, and 23.2% for placebo. Subjects experienced skeletal muscle tremor with both bitolterol mesylate (four subjects) and isoproterenol (three subjects), but not with placebo. No other side effects were noted.

Adolescent↗
PubMed1996

Pharmacokinetics of the active metabolite (MDL 74,156) of dolasetron mesylate after oral or intravenous administration to anesthetized children.

BACKGROUND: Dolasetron mesylate is a selective 5-HT3 receptor antagonist under investigation as an antiemetic in children. Published studies indicate that its antiemetic activity results from the active metabolite (MDL 74,156), which is produced within 10 minutes of administration of dolasetron mesylate. METHODS: The pharmacokinetics of MDL 74,156 and the safety and tolerability of dolasetron mesylate were studied after a single oral or intravenous dose of 1.2 mg.kg-1 dolasetron mesylate to healthy children from 2 to 12 years of age. Oral dolasetron was administered to 12 children 1 to 2 hours before anesthesia. Intravenous dolasteron was administered to 18 children at induction of anesthesia. Serial blood samples were collected for 24 hours after dosing to measure the plasma concentration of MDL 74,156. Indexes of liver and kidney function were determined, and electrocardiograms and adverse events were recorded.

Administration, Oral↗
PubMed2004

NiCl(2)(dppe)-catalyzed cross-coupling of aryl mesylates, arenesulfonates, and halides with arylboronic acids.

An investigation of the NiCl(2)(dppe)-, NiCl(2)(dppb)-, NiCl(2)(dppf)-, NiCl(2)(PCy(3))(2)-, and NiCl(2)(PPh(3))(2)-catalyzed cross-coupling of the previously unreported aryl mesylates, and of aryl arenesulfonates, chlorides, bromides, and iodides containing electron-withdrawing and electron-donating substituents with aryl boronic acids, in the absence of a reducing agent, is reported. NiCl(2)(dppe) was the only catalyst that exhibited high and solvent-independent activity in the two solvents investigated, toluene and dioxane. NiCl(2)(dppe) with an excess of dppe, NiCl(2)(dppe)/dppe, was reactive in the cross-coupling of electron-poor aryl mesylates, tosylates, chlorides, bromides, and iodides. This catalyst was also efficient in the cross-coupling of aryl bromides and iodides containing electron-donating substituents. Most surprisingly, the replacement of the excess dppe from NiCl(2)(dppe)/dppe with excess PPh(3) generated NiCl(2)(dppe)/PPh(3), which was found to be reactive for the cross-coupling of both electron-rich and electron-poor aryl mesylates and chlorides. Therefore, the solvent-independent reactivity of NiCl(2)(dppe) provides an inexpensive and general nickel catalyst for the cross-coupling of aryl mesylates, tosylates, chlorides, bromides, and iodides with aryl boronic acids.

Journal Article↗
PubMed1996

Moisture-dependent crystallization of amorphous lamotrigine mesylate.

A commercially available computer-controlled vacuum moisture balance was used for determining moisture sorption isotherms of freeze-dried and spray-dried lamotrigine mesylate drug substance and freeze dried drug product containing mannitol. The presence or absence of desorption hysteresis and the characteristics of the weight-versus-time profile as a sample was exposed to a defined relative humidity ramp were sensitive indicators of moisture-induced crystallization. Combination of the moisture sorption data with polarized light microscopy, differential scanning calorimetry, and X-ray powder diffraction provided qualitative verification of the crystallization with < 50 mg of sample. The normalized water loss during crystallization was used to detect as little as 2% amorphous content in physical mixtures of amorphous and crystalline lamotrigine mesylate. Moisture sorption, water plasticization, and crystallization properties of amorphous forms prepared by spray drying and freeze drying were nearly identical. Cofreeze-drying lamotrigine mesylate with D-mannitol resulted in a mixture of amorphous lamotrigine mesylate with properties similar to those of spray-dried or freeze-dried materials and crystalline D-mannitol. The amount of water needed for crystallization over a time scale observable in the moisture balance was considerably more than the amount needed to lower the glass transition temperature of the sample to the operating temperature of the instrument. This result illustrated the importance of time scale effects in determining critical moisture levels for crystallization from the amorphous state.

Crystallization↗
PubMed2002

Long-term safety and efficacy of oral phentolamine mesylate (Vasomax) in men with mild to moderate erectile dysfunction.

The objectives of this study were to evaluate long-term safety and efficacy of phentolamine mesylate, an orally active, rapid-acting alpha-adrenergic receptor antagonist, for the treatment of men suffering from erectile dysfunction (ED). It was an open-label study involving more than 2000 patients. Men received phentolamine mesylate 40 mg or 80 mg (10 tablets/month) as needed for up to 13 months and self-assessed erectile performance using two validated questionnaires. Treatment with phentolamine mesylate was associated with increases in Erectile Function Domain score of the IIEF, successful vaginal penetrations, and in overall satisfaction. Most adverse events were mild or moderate in severity and consistent with the known pharmacodynamic properties of phentolamine. In conclusion, phentolamine mesylate is safe and effective in the long-term treatment of men with mild to moderate ED.

Administration, Oral↗
PubMed1976

A comparison of the effects of CB-154 and lergotrile mesylate on prolactin and growth hormone secretion in mice.

The influence of 2-bromo-alpha-ergocryptine (CB-154) and 2-chloro-6-methyl-ergoline-8beta-acetonitrile methanesulfonate (lergotrile mesylate) on prolactin (PRL) and growth hormone (GH) secretion in mice was investigated. Both drugs inhibited the nursing-induced rise in serum PRL in lactating mice, CB-154 being effective at a somewhat lower dosage than lergotrile mesylate. Both drugs reduced basal concentrations of serum PRL by more than 90% within an hr after administration, but the effect of CB-154 lasted for several hr longer than that of lergotrile mesylate. CB-154 did not change the resting concentrations of GH in mice, but it promoted the induction of GH release by nursing; injection of lergotrile mesylate, on the other hand, seemed to enhance the basal concentrations of GH in lactating mice that were separated from their young for 12 hr. The results show that both drugs can be used successfully for reducing PRL secretion in the mouse.

Acetonitriles↗
PubMed2002

Stability of fenoldopam mesylate in two infusion solutions.

The physical and chemical stability of fenoldopam as the mesylate salt were studied. Test samples of fenoldopam mesylate, with fenoldopam concentrations ranging from 4 to 300 micrograms/mL, were prepared in polyvinyl chloride (PVC) bags of 5% dextrose injection and 0.9% sodium chloride injection and were stored at 4 degrees C in the dark and 23 degrees C in ambient fluorescent light. Physical and chemical stability were evaluated at 0, 24, 48, and 72 hours. Physical stability was assessed by visual observation in fluorescent light and using a high-intensity monodirectional light beam. Turbidity and particle content were measured electronically. Chemical stability of fenoldopam mesylate was evaluated by using a stability-indicating high-performance liquid chromatographic analytical technique. All samples were physically stable throughout the study. Little or no change in particulate burden and haze level was found. Little or no loss of fenoldopam occurred in concentrations of 40 micrograms/mL or greater at either temperature throughout the study period. At the lowest concentrations, minor losses of 3-5% were found. Fenoldopam mesylate, prepared in fenoldopam concentrations ranging from 4 to 300 micrograms/mL, was physically and chemically stable in PVC bags of 5% dextrose and 0.9% sodium chloride injections for 72 hours when stored at 4 degrees C in the dark and 23 degrees C when exposed to ambient fluorescent light.

Chromatography, High Pressure Liquid↗
PubMed1994

Lewis rat EAN is suppressed by the 21-aminosteroid tirilazad mesylate (U-74006F).

Lewis rat experimental allergic neuritis (EAN) was treated with the 21-aminosteroid, tirilazad mesylate (U-74006F). High doses of tirilazad mesylate, begun just before the onset of clinical signs, reduced the clinical and pathological severity of the disease. In rats immunized with a high dose of myelin, axonal degeneration was a major pathological feature. Tirilazad mesylate reduced the amount of axonal degeneration but had little effect on the other pathological features of EAN, such as inflammation and demyelination. Tirilazad mesylate may block axonal degeneration by inhibiting lipid peroxidation of axonal membranes. Inhibition of axonal degeneration is an important goal in the treatment of human neuropathies.

Animals↗
PubMed2001

Renal blood flow changes induced with endothelin-1 and fenoldopam mesylate at quantitative Doppler US: initial results in a canine study.

PURPOSE: To evaluate quantitative Doppler ultrasonography (US) for assessing renal blood flow changes induced with endothelin-1 (ET-1) and fenoldopam mesylate in conscious dogs. MATERIALS AND METHODS: A blood flow probe was surgically implanted around the renal artery in eight adult dogs. Color and power Doppler US images were acquired in conscious restrained dogs during intravenous infusion of ET-1 and fenoldopam mesylate. Simultaneous with imaging, blood flow through the renal artery was measured with the implanted probe. The color level of the images within the region representing the kidney was analyzed to derive flow indices. These indices were compared with direct-flow measurements. RESULTS: The flow indices, color-weighted flow area (CWFA), and percentage of area of color, derived from color and power Doppler US images, correlated linearly with direct flow. The mean color level of color and power Doppler US images correlated weakly with direct flow. Pre- versus postinfusion CWFA decreased with all ET-1 infusions (P < or =.032). Infusion of fenoldopam mesylate increased CWFA in all cases (P < or =.032). CONCLUSION: Quantitative Doppler US enabled successful measurement of the flow changes induced with ET-1 and fenoldopam mesylate. Quantitative Doppler US is potentially useful as a noninvasive surrogate endpoint in evaluating the action of various therapeutic agents.

Animals↗