Molecular Formula | C27H30F6N2O2 |
Molar Mass | 528.53 |
Density | 1.303±0.06 g/cm3(Predicted) |
Melting Point | 242-250°C |
Boling Point | 620.3±55.0 °C(Predicted) |
Flash Point | 328.954°C |
Solubility | DMSO: soluble2mg/mL, clear |
Vapor Presure | 0mmHg at 25°C |
Appearance | powder |
Color | white to beige |
pKa | 13.32±0.70(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.523 |
Physical and Chemical Properties | Melting point 242-250°C |
HS Code | 2937290000 |
Introduction | dutaperide is a novel dual inhibitor of 5α reductase, it inhibits both 5α-reductase -1 and 5α-reductase -2. It reduced the concentration of DHT more than finasteride (94. 7% vs. 70. 8%). The inhibitory effect of dutoxeride on 5α-reductase -1 is 60 times that of finasteride. Twenty-seven months after taking dutam, Incidence Rate of prostate cancers were 50% lower than in the placebo group. |
indication | dutaperide can be used to treat moderate to severe symptoms of benign prostatic hyperplasia (BPH). For patients with moderate to severe symptoms of benign prostatic hyperplasia, reduce the risk of acute urinary retention (AUL) and surgery. |
drug interaction | the metabolism of duptamil in the liver by CYP3A4, in vitro experiments showed that CYP3A4 inhibitory drugs such as ritonavir, ketoconazole, verapamil, diltiazem, cimetidine, and ciprofloxacin increased plasma concentrations of moderate tapiocin, whereas tamsulosin, terazosin, there is no pharmacological and pharmacokinetic interaction between warfarin and colestamide. |
treatment of benign prostatic hyperplasia drug | on 9 October 2002, a new drug, dutaglinamide, successfully developed by GlaxoSmithKline, was approved by the U. S. Food and Drug Administration for the treatment of prostate enlargement. on 19 June 2008, GlaxoSmithKline announced the FDA approval of dutaasteride (Avodart) in combination with tamsulosin (Harnal) for the treatment of benign prostatic hyperplasia. In China, on average, every two elderly men over 60 years old have a benign prostatic hyperplasia, which can cause lower urinary tract symptoms, including significantly increased frequency of urination, weak urine flow, and difficulty in bladder emptying, as well as nocturia, and even cause serious complications including acute urinary retention, reduce the patient's quality of life, affect the social life. dutaperide is the first and only dual 5α-reductase inhibitor for the treatment of benign prostatic hyperplasia, which improves urinary symptoms and reduces the risk of acute urinary retention episodes and associated prostate surgery. Tamsulosin is an alpha receptor blocker and can improve the symptoms of prostatic hyperplasia. There are two types of 5α reductase in human body: type I and type II. Type II mainly exists in prostate, and type I is mainly distributed in liver and skin. 5α reductase is an important reason for the progression of benign prostatic hyperplasia disease, which can promote the conversion of testosterone in the prostate of patients to the more active dihydrotestosterone, which leads to the hyperplasia of prostate cells and the hypertrophy of prostate gland. Therefore, the key to the treatment of benign prostatic hyperplasia is the inhibition of 5α reductase. Dutaperide can inhibit both type I and Type II 5 alpha reductase, through this 'dual repression' mechanism, dutaperide can rapidly and continuously reduce the prostate volume, significantly Improve lower urinary tract symptoms, reduce acute urinary retention and associated risk of prostate surgery, so that patients with sustained benefit, especially in the majority of patients with moderate and severe benign prostatic hyperplasia. |
clinical evaluation | FDA approval based on a 2-year multicenter, randomized, double-blind, controlled clinical study-the first long-term evaluation clinical study on the combination of amine and alpha receptor blocker. Enrolled patients were men with moderate to severe prostatic hyperplasia (age greater than or equal to 50 years, prostate volume (PV)≥ 30CC, serum prostate specific antigen (PSA)). 1.5 ~ 10ng/mL,5mL/s |
Use | Dutasteride is a 5 alpha-reductase inhibitor. |