Imatinib mesylate has been commonly used in the treatment of patients with chronic myeloid leukemia (CML). However, a significant number of CML patients treated with imatinib developed thrombocytopenia, oligocythemia, granulocytopenia. It has been confirmed that imatinib not only inhibits BCR-ABL mutations, but also suppresses other tyrosine kinase receptor genes such as PDGFR, JAK2V617F and C-KIT mutations, providing an important potential of targeted therapy for myeloproliferative disease. As the PDGFR, JAK2 and C-KIT play important roles in the regulation of hematopoiesis, suggesting that imatinib may block the phosphorylation of PDGFR, JAK2V617F and C-KIT receptors, interrupt the signal transduction cascades, disrupt cell differentiation and proliferation. In this review, the application and the potential molecular mechanism of imatinib in the treatment of thrombocythemia and other myeloproliferative diseases are discussed.
Benzamides ; therapeutic use ; Humans ; Imatinib Mesylate ; Myeloproliferative Disorders ; drug therapy ; Piperazines ; therapeutic use ; Pyrimidines ; therapeutic use ; Thrombocytosis ; drug therapy

OBJECTIVETo observe the clinical efficacy of self-formulated Xingchang Decoction (XCD) in treating slow-transit constipation (STC) and the dynamical parameters of colonic motility during XCD treatment.

METHODSOne hundred and eighteen patients with STC were randomly assigned to the treatment group and the control group, 59 in each group. The treatment group was treated with XCD, and the control group was treated with mosapride, an intestinal energetic agent. The therapeutic course for both groups was 30 days. The 72-h colonic transition test was conducted and the symptom scores were observed before and after treatment; the adverse reaction rate and clinical efficacy were calculated after treatment; and the recurrence rate in one year was followed-up.

RESULTSSymptom scores were significantly improved in the treatment group after treatment, with the improvement significantly superior to that in the control group (P < 0.01). The cure rate and the total effective rate were 76.27% and 93.22% in the treatment group respectively, while they were 47.45% and 72.87% in the control group, showing significant difference between the two groups (P < 0.01). Besides, the 1-year recurrence rate was significantly lower (chi2 = 10.40, P = 0.001) and the improvement of colonic motor function was more in the treatment group than those in the control group (P < 0.01). Only low incidence (5.08% in the treatment group and 8.47% in the control group) of mild gastrointestinal reactions was shown, which caused no influence on the treatment.

CONCLUSIONXCD could effectively improve the motility of the digestive tract, and it is effective and safe for the treatment of STC.

Benzamides ; therapeutic use ; Constipation ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Gastrointestinal Agents ; therapeutic use ; Gastrointestinal Transit ; drug effects ; Humans ; Morpholines ; therapeutic use

OBJECTIVE: To explore the relevance between nasal symptoms and laryngopharyngeal reflux disease in patients with allergic rhinitis. METHOD: Thirty patients of laryngopharyngeal reflux disease were diagnosed in ENT outpatient department in our hospital. All patients have symptoms of sneeze, nasal discharge as chief complaint and they responded no effect for other normal treatment for nasal-sinusitis at least three months. Orally before meals, a dose of 5 mg Mosapride citrate each time, three times a day for 7 days. Orally before meals, a dose of 20 mg Esomeprazole each time, two times a. day for 2-3 months. Nasal spray, one spray of azelastine hydrochloride once, two times a day for 2 month. RESULT: Laryngopharyngeal reflux symptom scores at four time points (the first visit, post treatment 15 days, 45 days, 75 days) were analyzed by repeated measures analysis of variance. There is a significant difference in four time points. CONCLUSION Laryngopharyngeal reflux disease has a strong association with allergic rhinitis. Patients who has allergic rhinitis nasal symptoms as chief complaint must be exclude, the laryngopharyngeal reflux disease first.
Benzamides ; therapeutic use ; Esomeprazole ; therapeutic use ; Humans ; Laryngopharyngeal Reflux ; complications ; drug therapy ; Morpholines ; therapeutic use ; Phthalazines ; therapeutic use ; Pilot Projects ; Rhinitis, Allergic ; drug therapy ; etiology

Gastrointestinal stromal tumor(GIST) originates from interstitial cells of Cajal(ICCs). Tyrosine kinase inhibitors(TKI) such as imatinib and sunitinib, are effective agents besides surgery. However some GIST can become primarily or secondarily resistant to those drugs. The difference in gene mutation types and secondary gene mutation is the main cause. When the GIST is proved to be drug resistance, reasonable personal treatment strategies based on individualized medicine should be made to improve outcomes and quality of life.
Antineoplastic Agents ; therapeutic use ; Benzamides ; therapeutic use ; Drug Resistance, Neoplasm ; genetics ; Gastrointestinal Stromal Tumors ; drug therapy ; genetics ; Humans ; Imatinib Mesylate ; Indoles ; therapeutic use ; Piperazines ; therapeutic use ; Protein Kinase Inhibitors ; therapeutic use ; Pyrimidines ; therapeutic use ; Pyrroles ; therapeutic use

Currently, the treatment of recurrent or metastatic gastrointestinal stromal tumor(GIST) has become a tremendous challenge. Some international clinical trials revealed that imatinib might significantly improve the survival of patients with recurrent or metastatic GIST. Though the combination of surgery and imatinib has become an ideal treatment of metastatic GIST, there still exist some controversies regarding how to combine the two methods. Imatinib may influence the blood coagulation mechanism, therefore it is suggested that imatinib cessation should be performed a week before operation. Cytoreductive surgery has some clinical effects on recurrent or metastatic GIST, which can be combined with targeted therapy. Furthermore, the clinical trial for recurrent or metastatic GIST needs further evaluation.
Benzamides ; administration & dosage ; therapeutic use ; Combined Modality Therapy ; Gastrointestinal Stromal Tumors ; drug therapy ; surgery ; Humans ; Imatinib Mesylate ; Piperazines ; administration & dosage ; therapeutic use ; Pyrimidines ; administration & dosage ; therapeutic use

OBJECTIVETo evaluate the effectiveness and safety of mosapride on treatment of functional dyspepsia.

METHODSRandomized controlled clinical trial was conducted and patients suffered from functional dyspepsia were included. 5 mg mosapride was given three times daily for 4 weeks in the treatment group. 10 mg domperidone was given three times daily for 4 weeks as control. Changes on symptom score, gastric empty or new occurring events were included as outcomes.

RESULTS231 patients suffered from functional dyspepsia were selected by inclusion and exclusion criteria from August 15 to Oct 22, 1999. Of these, 108 (46.8%) were males, versus 123 (53.2%) females and 118 (51.2%) in the treatment group and 113 (48.9%) as controls. 222 (96.1%) patients were followed up. Results showed that the total efficacy rates in early satiety and abdominal distension were 84.5% and 90.1% in mosapride after the 2 weeks of treatment. Mosapride seemed to be more effective in improving symptoms of belching and heartburn than that in controls (P < 0.05). In 4 weeks, the total efficacy in improving symptoms of abdominal distention and belching showed more effective in mosapride than that in controls (P < 0.05). Decrease of symptoms score was more in mosapride than that in controls (P < 0.05). Mosapride was less effective in controls in improving the gastric empty in terms of proportion (46.2% vs. 25.9%, P = 0.020) and range (46.2% vs. 24.0%, P = 0.003). Side effects would include diarrhea, constipation, headache, dizziness, insomnia, skin scare and the like. There was no significant difference between the two groups (9.6% in mosapride vs. 14.0% in controls).

CONCLUSIONMosapride was safe and effective in improving the symptoms and gastric empty of functional dyspepsia.

Adult ; Benzamides ; adverse effects ; therapeutic use ; Dyspepsia ; drug therapy ; Female ; Gastrointestinal Agents ; adverse effects ; therapeutic use ; Humans ; Male ; Middle Aged ; Morpholines ; adverse effects ; therapeutic use ; Treatment Outcome

OBJECTIVETo explore demographic characteristics, current diagnosis and treatment patterns of chronic myelogenous leukemia (CML) patients in China.

METHODSData of hospitalized CML patients in 2005 whole year and outpatient information (July 1 through September 30, 2006) from 15 hospitals throughout China were analyzed.

RESULTSA total of 1824 CML cases were analyzed, including 722 inpatients and 1102 outpatients. The male/female ratio was 1.78:1. The median age at diagnosis was 40.02 (2.45 - 83.29) years old, 90.41% of the patients were diagnosed at chronic phase. Proportion of accelerated phase or blast crisis patients increased to 21.66% during study period. 93.20% of the patients received blood routine and bone marrow morphologic examination at diagnosis and in monitoring; 70.29% were performed cytogenetic analysis and 51.54% performed molecular measurement in addition. The most common therapy for CML treatment was hydroxycarbamide. The proportion of patients treated with imatinib and interferon was 37.45% and 25.55%, respectively. Of 722 inpatients, 164 (22.72%) received hemotopoietic stem cell transplantation (HSCT). The proportions of accelerated phase and blast crisis patients treated with imatinib were 48.28% and 48.42%, respectively, being significantly higher than that of chronic phase patients (35.9%) (P < 0.05). The mean imatinib dosage administered in the three phases patients did not differ significantly. Imatinib resistance rates were 6.87% and 16.28% for outpatient and inpatient, respectively. In the outpatient group, the primary resistance to imatinib occurred comparably to the secondary resistance (68.75%), while primary resistance was predominant in inpatient group (65.71%). The intolerance rates of imatinib for outpatient and inpatient were 3.21%, 11.63%, respectively. The majority of patients treated with imatinb were not monitored in time: 63.38% patients evaluated hematologic response after 3 months of treatment, proportions of patients received cytogenetic examination after 6 months and 12 months of treatment were 41.41% and 27.35%, respectively. Mean cost for HSCT was 213 092 +/- 125 890 RMB.

CONCLUSIONSCML in China tends to afflict younger population than in Western countries. Most patients were diagnosed in the chronic phase. Due to restriction of financial support, only one third of CML patients were treated with imatinib, and the majority of the treated were not monitored in time. Clinicians should pay attention to resistance and intolerance to imatinib treatment in accelerated phase or blast crisis patients.

Benzamides ; therapeutic use ; China ; Humans ; Imatinib Mesylate ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive ; drug therapy ; Piperazines ; therapeutic use ; Pyrimidines ; therapeutic use

Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tumor of the gastrointestinal tract. Its pathogenesis is defined by mutations within the KIT and PDGFRα gene. Surgical resection is the only radical treatment at present, but recurrence is common. In recent years, targeted therapy with imatinib mesylate, which inhibits KIT kinase activity, represents the other cornerstone for the treatment of GIST. For resectable GIST, operation combined with neoadjuvant and adjuvant therapy with imatinib mesylate or other tyrosine kinase inhibitors can improve the prognosis of high-risk patients before or after complete resection. For unresectable GIST, targeted therapy with imatinib mesylate can effectively inhibit and ameliorate the progression of GIST.
Benzamides ; therapeutic use ; Gastrointestinal Neoplasms ; drug therapy ; surgery ; therapy ; Gastrointestinal Stromal Tumors ; drug therapy ; surgery ; therapy ; Humans ; Imatinib Mesylate ; Piperazines ; therapeutic use ; Pyrimidines ; therapeutic use

Gastrointestinal stromal tumor (GIST) represents the most common mesenchymal tumor of the gastrointestinal tract. With decades of development, surgical excision combined with molecular targeted agents is becoming the mode for the GIST treatment. Imatinib mesylate (IM) is the first-line therapy medicine for GIST adjuvant treatment, and it significantly reduces recurrence or metastasis and increases survival. According to the recently results of SSGXVIII/AIO study, imatinib adjuvant therapy should be administered for at least 3 years for the GIST patients with a high estimated risk of recurrence and metastasis after surgery. Nevertheless, the optimal duration of the adjuvant therapy or the follow-up policy remains unclear, and we look forward to standard assessment criteria for individualized treatment.
Benzamides ; therapeutic use ; Chemotherapy, Adjuvant ; Gastrointestinal Neoplasms ; drug therapy ; surgery ; Gastrointestinal Stromal Tumors ; drug therapy ; surgery ; Humans ; Imatinib Mesylate ; Piperazines ; therapeutic use ; Pyrimidines ; therapeutic use

PROSPER is an international Phase III trial demonstrating the beneficial role of enzalutamide, an androgen receptor antagonist, in prolonging metastasis-free survival in men with nonmetastatic castration-resistant prostate cancer. The trial showed that the median metastasis-free survival was 21.9 months longer for those treated with enzalutamide (36.6 months) compared to those treated with placebo (14.7 months). Enzalutamide also showed prolonged time to PSA progression, PSA response, and time to initiating additional antineoplastic therapy although overall survival is not yet reached. Enzalutamide is the second antiandrogen (next to apalutamide) that has gained the United States Food and Drug Administration (US FDA) label indication for use in the setting of nonmetastatic castration-resistant prostate cancer.
Androgen Antagonists/therapeutic use* ; Antineoplastic Agents/therapeutic use* ; Benzamides ; Humans ; Male ; Nitriles ; Phenylthiohydantoin/therapeutic use* ; Prostatic Neoplasms, Castration-Resistant/drug therapy*