美国FDA近日已批准Noxafil (posaconazole，泊沙康唑) 口服混悬剂上市，用于治疗13岁以上人群的曲霉菌、假丝酵母菌的入侵性感染。入侵性真菌感染能威胁生命，通常发生在免疫力受抑制的病人中，如：器官移植病人，干细胞移植及接受化疗的癌症患者。 Noxafil是FDA首次批准用于治疗由曲霉菌引起的入侵性真菌感染的抗真菌药物。Noxafil由先灵葆雅公司研发，在2005年10月已欧洲获得批准用于成人严重入侵性真菌感染。 商品名 Noxafil 开发与上市厂商 本品由先灵葆雅公司（Scher- ing-Plough)开发，2005年12月在德国首次上市，2006年3月在英国上市。 适应证 本品适用于多种对两性霉素B 不耐受或难治性成人侵袭性真菌感染的治疗。 药理作用 本品抑制细胞色素P450(CYP) 的14-α-脱甲基酶，对霉菌和酵母菌具有广谱抗菌活性。本品临床空腹或餐后口服，分别在3～4小时和4 ～10小时达血浆峰浓度。本品可透过胎盘屏障，且在乳汁中有分泌。临床研究显示，本品血浆蛋白结合率高达98.2%，主要与白蛋白结合。 本品临床表观分布容积达744 ～5845L（平均1744L），提示本品具有高度组织穿透力。 本品平均清除半衰期为(t1/2)35 小时，全身总清除率为32 L/hr。 本品主要随粪清除（占放射性标记给药剂量的71％），且大部分以母体药物形式排出（占放射性标记给药剂量的66%）。肾清除是本品的次要消除途径，约占放射性标记给药剂量的13%，其中母体药物低于放射性标记给药剂量的0.2％。 临床评价 一项在485例患有口咽部念珠菌病的HIV阳性患者中进行的多中心随机双盲Ⅱ期临床研究显示，口服本品50、100、200和400mg与口服氟康唑100mg一样安全有效，且耐受性均良好。本品不同剂量的临床有效率分别为85%、87%、77% 和87%，而氟康唑为87%；本品各剂量的真菌灭除率分别为36％、 37％、35%和40%，而氟康唑为 50%。 2007年1月出版的The New England Journal of Medicine刊载 7先灵葆雅公司(Schering-Plough) 报道的2项意义重大的本品预防侵袭性真菌感染的临床研究结果。此 2项临床研究显示，本品口服混悬剂可有效预防高危患者中曲霉菌和念珠菌引起的致死性侵袭性真菌感染，其中一项研究提示患者总死亡率降低，与对照药物氟康唑（flucon- azole）和伊曲康唑（itraconazole）相比，本品能更有效预防侵袭性曲霉菌感染并可降低侵袭性真菌感染相关的死亡率。 不良反应 本品最常见的治疗相关性严重不良反应有胆红素血症、肝脏酶升高、肝细胞损害以及恶心和呕吐。临床研究中罕见有肝脏反应。 注意事项 对本品或任一组分过敏者禁用本品。本品不宜与麦角生物碱合用，不宜与CYP3A4底物特非那定、阿司咪唑、西沙必利、匹莫齐特、卤泛群或奎尼丁合用，因合用后会使这些药物的血浆浓度上升，从而导致QTc延长和罕见的尖端扭转型（室性）心动过速。本品不宜与辛伐他汀、洛伐他汀及阿托伐他汀等合用。 用法与用量 本品推荐剂量为一日2次，每次400m g(1Om L)，随餐服用或随 240mL营养补充剂服用。 制剂 口服混悬剂，剂量规格为 40mg/mL。 FDA接受先灵葆雅泊沙康唑的新药申请　 FDA已接受先灵葆雅公司的口服广谱三唑类抗真菌药泊沙康唑(posaconazole,Noxafil)的新药申请，申请中提供了337例病人的研究资料。泊沙康唑用于难治性疾病或其他药物耐药引起的真菌感染，即曲霉病、镰刀菌病和接合菌病。此种感染一般发生在有免疫损害的病人身上，例如器官移植或进行化疗的病人。在提交的申请中也寻求对泊沙康唑显示有治疗活性的严重呼吸道真菌病球孢子菌病的准许。 NOXAFIL 40 mg/ml oral suspension Drug Class Description : Antimycotics for systemic use-triazole derivatives Generic Name : Posaconazole Drug description : Each ml of oral suspension contains 40 mg of posaconazole. Presentation : Oral suspension White suspension Indications : Noxafil is indicated for use in the treatment of the following fungal infections in adults - Invasive aspergillosis in patients with disease that is refractory to amphotericin B or itraconazole or in patients who are intolerant of these medicinal products; - Fusariosis in patients with disease that is refractory to amphotericin B or in patients who are intolerant of amphotericin B; - Chromoblastomycosis and mycetoma in patients with disease that is refractory to itraconazole or in patients who are intolerant of itraconazole; - Coccidioidomycosis in patients with disease that is refractory to amphotericin B, itraconazole or fluconazole or in patients who are intolerant of these medicinal products; - Oropharyngeal candidiasis: as first-line therapy in patients who have severe disease or are immunocompromised, in whom response to topical therapy is expected to be poor. Refractoriness is defined as progression of infection or failure to improve after a minimum of 7 days of prior therapeutic doses of effective antifungal therapy. Noxafil is also indicated for prophylaxis of invasive fungal infections in the following patients: - Patients receiving remission-induction chemotherapy for acute myelogenous leukemia (AML) or myelodysplastic syndromes (MDS) expected to result in prolonged neutropenia and who are at high risk of developing invasive fungal infections; - Hematopoietic stem cell transplant (HSCT) recipients who are undergoing high-dose immunosuppressive therapy for graft versus host disease and who are at high risk of developing invasive fungal infections. Adult Dosage : Treatment should be initiated by a physician experienced in the management of fungal infections or in the supportive care in the high risk patients for which posaconazole is indicated as prophylaxis. Recommended dosage is shown in Table 1. Table 1. Recommended dose according to indication Indication Dose and duration of therapy Refractory Invasive Fungal Infections (IFI)/Intolerant patients with IFI 400 mg (10 ml) twice a day. In patients who cannot tolerate a meal or a nutritional supplement, Noxafil should be administered at a dose of 200 mg (5 ml) four times a day. Duration of therapy should be based on the severity of the underlying disease, recovery from immunosuppression, and clinical response. Oropharyngeal Candidiasis Loading dose of 200 mg (5 ml) once a day on the first day, then 100 mg (2.5 ml) once a day for 13 days. Each dose of Noxafil should be administered with a meal, or with a nutritional supplement in patients who cannot tolerate food to enhance the oral absorption and to ensure adequate exposure. Prophylaxis of Invasive Fungal Infections 200 mg (5 ml) three times a day. Each dose of Noxafil should be administered with a meal, or with a nutritional supplement in patients who cannot tolerate food to enhance the oral absorption and to ensure adequate exposure. The duration of therapy is based on recovery from neutropenia or immunosuppression. For patients with acute myelogenous leukemia or myelodysplastic syndromes, prophylaxis with Noxafil should start several days before the anticipated onset of neutropenia and continue for 7 days after the neutrophil count rises above 500 cells per mm3 . There are limited pharmacokinetic data in patients with severe gastrointestinal dysfunction (such as severe diarrhoea). Patients who have severe diarrhoea or vomiting should be monitored closely for breakthrough fungal infections. The oral suspension must be shaken well before use. Use in renal impairment: An effect of renal impairment on the pharmacokinetics of posaconazole is not expected and no dose adjustment is recommended. Use in hepatic impairment: There are limited pharmacokinetic data in patients with hepatic impairment; therefore, no recommendation for dose adjustment can be made. In the small number of subjects studied who had hepatic impairment, there was an increase in exposure and half-life with a decrease in hepatic function. Use in children: Safety and efficacy in children and adolescents below the age of 18 years have not been established. Therefore posaconazole is not recommended for use in patients below 18 years of age. Child Dosage : Safety and efficacy in children and adolescents below the age of 18 years have not been established. Therefore posaconazole is not recommended for use in patients below 18 years of age. Elderly Dosage : See Adult Dosage Contra Indications : Hypersensitivity to the active substance or to any of the excipients. Co-administration with ergot alkaloids. Co-administration with the CYP3A4 substrates terfenadine, astemizole, cisapride, pimozide, halofantrine or quinidine since this may result in increased plasma concentrations of these medicinal products, leading to QTc prolongation and rare occurrences of torsades de pointes. Co-administration with the HMG-CoA reductase inhibitors simvastatin, lovastatin and atorvastatin. Special Precautions : Hypersensitivity: There is no information regarding cross-sensitivity between posaconazole and other azole antifungal agents. Caution should be used when prescribing Noxafil to patients with hypersensitivity to other azoles. Hepatic toxicity: Hepatic reactions (e.g. mild to moderate elevations in ALT, AST, alkaline phosphatase, total bilirubin and/or clinical hepatitis) have been reported during treatment with posaconazole. Elevated liver function tests were generally reversible on discontinuation of therapy and in some instances these tests normalised without interruption of therapy. Rarely, more severe hepatic reactions with fatal outcomes have been reported. Posaconazole should be used with caution in patients with severe hepatic impairment. In these patients, the prolonged elimination half-life may lead to increased exposure. Monitoring of hepatic function: Patients who develop abnormal liver function tests during Noxafil therapy must be routinely monitored for the development of more severe hepatic injury. Patient management should include laboratory evaluation of hepatic function (particularly liver function tests and bilirubin). Discontinuation of Noxafil should be considered if clinical signs and symptoms are consistent with development of liver disease. QTc prolongation: Some azoles have been associated with prolongation of the QTc interval. Noxafil must not be administered with medicinal products that are substrates for CYP3A4 and are known to prolong the QTc interval. Noxafil should be administered with caution to patients with pro-arrhythmic conditions such as: • Congenital or acquired QTc prolongation • Cardiomyopathy, especially in the presence of cardiac failure • Sinus bradycardia • Existing symptomatic arrhythmias • Concomitant use with medicinal products known to prolong the QTc interval. Electrolyte disturbances, especially those involving potassium, magnesium or calcium levels, should be monitored and corrected as necessary before and during posaconazole therapy. Posaconazole is an inhibitor of CYP3A4 and should only be used under specific circumstances during treatment with other medicinal products that are metabolised by CYP3A4. Rifabutin: Concomitant use with posaconazole should be avoided unless the benefit to the patient outweighs the risk. Rifamycin antibacterials (rifampicin, rifabutin), certain anticonvulsants (phenytoin, carbamazepine, phenobarbital, primidone), efavirenz and cimetidine: Posaconazole concentrations may be significantly lowered in combination; therefore, concomitant use with posaconazole should be avoided unless the benefit to the patient outweighs the risk. This medicinal product contains approximately 1.75 g of glucose per 5 ml of suspension. Patients with glucose-galactose malabsorption should not take this medicine. Interactions : Effects of other medicinal products on posaconazole: Posaconazole is metabolised via UDP glucuronidation (phase 2 enzymes) and is a substrate for p-glycoprotein (P-gp) efflux in vitro. Therefore, inhibitors (e.g. verapamil, ciclosporin, quinidine, clarithromycin, erythromycin, etc.) or inducers (e.g. rifampicin, rifabutin, certain anticonvulsants, etc.) of these clearance pathways may increase or decrease posaconazole plasma concentrations, respectively. Rifabutin (300 mg once a day) decreased the Cmax (maximum plasma concentration) and AUC (area under the plasma concentration time curve) of posaconazole to 57 % and 51 %, respectively. Concomitant use of posaconazole and rifabutin and similar inducers (e.g. rifampicin) should be avoided unless the benefit to the patient outweighs the risk. See also below regarding the effect of posaconazole on rifabutin plasma levels. Efavirenz (400 mg once a day) decreased the Cmax and AUC of posaconazole by 45 % and 50 %, respectively. Concomitant use of posaconazole and efavirenz should be avoided unless the benefit to the patient outweighs the risk. Phenytoin (200 mg once a day) decreased the Cmax and AUC of posaconazole by 41 % and 50 %, respectively. Concomitant use of posaconazole and phenytoin and similar inducers (e.g. carbamazepine, phenobarbital, primidone) should be avoided unless the benefit to the patient outweighs the risk. H2 receptor antagonists and proton pump inhibitors: Posaconazole plasma concentrations (Cmax and AUC) were reduced by 39 % when posaconazole was administered with cimetidine (400 mg twice a day) due to reduced absorption possibly secondary to a decrease in gastric acid production. Concomitant use of posaconazole and cimetidine should be avoided unless the benefit to the patient outweighs the risk. The effect of other H2 receptor antagonists (e.g. famotidine, ranitidine) and proton pump inhibitors (e.g. omeprazole) that may suppress gastric acidity for several hours on plasma levels of posaconazole has not been studied but a reduction in bioavailability may occur so that co-administration should be avoided if possible. Effects of posaconazole on other medicinal products: Posaconazole is a potent inhibitor of CYP3A4. Co-administration of posaconazole with CYP3A4 substrates may result in large increases in exposure to CYP3A4 substrates as exemplified by the effects on tacrolimus, sirolimus, atazanavir and midazolam below. Caution is advised during co-administration of posaconazole with CYP3A4 substrates administered intravenously and the dose of the CYP3A4 substrate may need to be reduced. If posaconazole is used concomitantly with CYP3A4 substrates that are administered orally, and for which an increase in plasma concentrations may be associated with unacceptable adverse events, plasma concentrations of the CYP3A4 substrate and/or adverse events should be closely monitored and the dose adjusted as needed. Several of the interaction studies were conducted in healthy volunteers in whom a higher exposure to posaconazole occurs compared to patients administered the same dose. The effect of posaconazole on CYP3A4 substrates in patients might be somewhat lower than that observed in healthy volunteers, and is expected to be variable between patients due to the variable posaconazole exposure in patients. The effect of co-administration with posaconazole on plasma levels of CYP3A4 substrates may also be variable within a patient, unless posaconazole is administered in a strictly standardised way with food, given the large food effect on posaconazole exposure. Terfenadine, astemizole, cisapride, pimozide, halofantrine and quinidine (CYP3A4 substrates): Co-administration of posaconazole and terfenadine, astemizole, cisapride, pimozide, halofantrine or quinidine is contraindicated. Co-administration may result in increased plasma concentrations of these medicinal products, leading to QTc prolongation and rare occurrences of torsades de pointes. Ergot alkaloids: Posaconazole may increase the plasma concentration of ergot alkaloids (ergotamine and dihydroergotamine), which may lead to ergotism. Co-administration of posaconazole and ergot alkaloids is contraindicated. HMG-CoA reductase inhibitors metabolised through CYP3A4 (e.g. simvastatin, lovastatin, and atorvastatin): Posaconazole may substantially increase plasma levels of HMG-CoA reductase inhibitors that are metabolised by CYP3A4. Treatment with these HMG-CoA reductase inhibitors should be discontinued during treatment with posaconazole as increased levels have been associated with rhabdomyolysis. Vinca alkaloids: Posaconazole may increase the plasma concentration of vinca alkaloids (e.g. vincristine and vinblastine), which may lead to neurotoxicity. Therefore, concomitant use of posaconazole and vinca alkaloids should be avoided unless the benefit to the patient outweighs the risk. If co-administered, then it is recommended that dose adjustment of vinca alkaloids be considered. Rifabutin: Posaconazole increased the Cmax and AUC of rifabutin by 31 % and 72 %, respectively. Concomitant use of posaconazole and rifabutin should be avoided unless the benefit to the patient outweighs the risk (see also above regarding the effect of rifabutin on plasma levels of posaconazole). If these medicinal products are co-administered, careful monitoring of full blood counts and adverse events related to increased rifabutin levels (e.g. uveitis) is recommended. Ciclosporin: In heart transplant patients on stable doses of ciclosporin, posaconazole 200 mg once daily increased ciclosporin concentrations requiring dose reductions. Cases of elevated ciclosporin levels resulting in serious adverse events, including nephrotoxicity and one fatal case of leukoencephalopathy, were reported in clinical efficacy studies. When initiating treatment with posaconazole in patients already receiving ciclosporin, the dose of ciclosporin should be reduced (e.g. to about three quarters of the current dose). Thereafter blood levels of ciclosporin should be monitored carefully during co-administration, and upon discontinuation of posaconazole treatment, and the dose of ciclosporin should be adjusted as necessary. Tacrolimus: Posaconazole increased Cmax and AUC of tacrolimus (0.05 mg/kg body weight single dose) by 121 % and 358 %, respectively. Clinically significant interactions resulting in hospitalisation and/or posaconazole discontinuation were reported in clinical efficacy studies. When initiating posaconazole treatment in patients already receiving tacrolimus, the dose of tacrolimus should be reduced (e.g. to about one third of the current dose). Thereafter blood levels of tacrolimus should be monitored carefully during co-administration, and upon discontinuation of posaconazole, and the dose of tacrolimus should be adjusted as necessary. Sirolimus: Repeat dose administration of oral posaconazole (400 mg twice daily for 16 days) increased the Cmax and AUC of sirolimus (2 mg single dose) an average of 6.7-fold and 8.9-fold (range 3.1 to 17.5-fold), respectively, in healthy subjects. The effect of posaconazole on sirolimus in patients is unknown, but is expected to be variable due to the variable posaconazole exposure in patients. Co-administration of posaconazole with sirolimus is not recommended and should be avoided whenever possible. If it is considered that co-administration is unavoidable, then it is recommended that the dose of sirolimus should be greatly reduced at the time of initiation of posaconazole therapy and that there should be very frequent monitoring of trough concentrations of sirolimus in whole blood. Sirolimus concentrations should be measured upon initiation, during co-administration, and at discontinuation of posaconazole treatment, with sirolimus doses adjusted accordingly. It should be noted that the relationship between sirolimus trough concentration and AUC is changed during co-administration with posaconazole. As a result, sirolimus trough concentrations that fall within the usual therapeutic range may result in sub-therapeutic levels. Therefore trough concentrations that fall in the upper part of the usual therapeutic range should be targetted and careful attention should be paid to clinical signs and symptoms, laboratory parameters and tissue biopsies. HIV Protease Inhibitors: As HIV protease inhibitors are CYP3A4 substrates, it is expected that posaconazole will increase plasma levels of these antiretroviral agents. Following co-administration of oral posaconazole (400 mg twice daily) with atazanavir (300 mg once daily) for 7 days in healthy subjects Cmax and AUC of atazanavir increased by an average of 2.6-fold and 3.7-fold (range 1.2 to 26-fold), respectively. Following co-administration of oral posaconazole (400 mg twice daily) with atazanavir and ritonavir (300/100 mg once daily) for 7 days in healthy subjects Cmax and AUC of atazanavir increased by an average of 1.5-fold and 2.5-fold (range 0.9 to 4.1-fold), respectively. The addition of posaconazole to therapy with atazanavir or with atazanavir plus ritonavir was associated with increases in plasma bilirubin levels. Frequent monitoring for adverse events and toxicity related to antiretroviral agents that are substrates of CYP3A4 is recommended during co-administration with posaconazole. Midazolam and other benzodiazepines metabolised by CYP3A4: In a study in healthy volunteers posaconazole (200 mg once daily for 10 days) increased the exposure (AUC) of IV midazolam (0.05 mg/kg) by 83 %. In another study in healthy volunteers, repeat dose administration of oral posaconazole (200 mg twice daily for 7 days) increased the Cmax and AUC of IV midazolam (0.4 mg single dose) by an average of 1.3- and 4.6-fold (range 1.7 to 6.4-fold), respectively; Posaconazole 400 mg twice daily for 7 days increased the IV midazolam Cmax and AUC by 1.6 and 6.2-fold (range 1.6 to 7.6-fold), respectively. Both doses of posaconazole increased Cmax and AUC of oral midazolam (2 mg single oral dose) by 2.2 and 4.5-fold, respectively. In addition, oral posaconazole (200 mg or 400 mg) prolonged the mean terminal half-life of midazolam from approximately 3-4 hours to 8-10 hours during co-administration. Due to the risk of prolonged sedation it is recommended that dose adjustments should be considered when posaconazole is administered concomitantly with any benzodiazepine that is metabolised by CYP3A4 (e.g. midazolam, triazolam, alprazolam). Calcium channel blockers metabolised through CYP3A4 (e.g. diltiazem, verapamil, nifedipine, nisoldipine): Frequent monitoring for adverse events and toxicity related to calcium channel blockers is recommended during co-administration with posaconazole. Dose adjustment of calcium channel blockers may be required. Digoxin: Administration of other azoles has been associated with increases in digoxin levels. Therefore, posaconazole may increase plasma concentration of digoxin and digoxin levels need to be monitored when initiating or discontinuing posaconazole treatment. Sulfonylureas: Glucose concentrations decreased in some healthy volunteers when glipizide was co-administered with posaconazole. Monitoring of glucose concentrations is recommended in diabetic patients. Adverse Reactions : The safety of posaconazole has been assessed in> 2,400 patients and healthy volunteers enrolled in clinical trials and from post-marketing experience. The most frequently reported serious related adverse reactions included nausea, vomiting, diarrhoea, pyrexia, and increased bilirubin. Within the organ system classes, adverse reactions are listed under headings of frequency using the following categories: very common (1/10); common (1/100 to <1/10); uncommon (1/1,000 to <1/100); rare ( 1/10,000 to <1/1,000); very rare (<1/10,000); not known.   Table 2. Adverse reactions by body system and frequency Blood and lymphatic system disorders Common: Uncommon: Rare:   neutropenia thrombocytopenia, leukopenia, anaemia, eosinophilia, lymphadenopathy haemolytic uraemic syndrome, thrombotic thrombocytopenic purpura, pancytopenia, coagulopathy, haemorrhage Immune system disorders Uncommon: Rare:   allergic reaction hypersensitivity reaction Endocrine disorders Rare:   adrenal insufficiency, blood gonadotropin decreased Metabolism and nutrition disorders Common: Uncommon:   electrolyte imbalance, anorexia hyperglycaemia Psychiatric disorders Rare: Not known:   psychotic disorder, depression confusional state Nervous system disorders Common: Uncommon: Rare:   paresthesia, dizziness, somnolence, headache convulsions, neuropathy, hypoaesthesia, tremor cerebrovascular accident, encephalopathy, peripheral neuropathy, syncope Eye disorders Uncommon: Rare:   blurred vision diplopia, scotoma Ear and labyrinth disorder Rare:   hearing impairment Cardiac disorders Uncommon: Rare:   long QT syndrome, electrocardiogram abnormal, palpitations torsade de pointes, sudden death, ventricular tachycardia, cardio-respiratory arrest, cardiac failure, myocardial infarction Vascular disorders Uncommon: Rare:   hypertension, hypotension pulmonary embolism, deep vein thrombosis Respiratory, thoracic and mediastinal disorders Rare:   pulmonary hypertension, interstitial pneumonia, pneumonitis Gastrointestinal disorders Common: Uncommon: Rare:   vomiting, nausea, abdominal pain, diarrhoea, dyspepsia, dry mouth, flatulence pancreatitis gastrointestinal haemorrhage, ileus Hepatobiliary disorders Common: Uncommon: Rare:   liver function tests raised (ALT increased, AST increased, bilirubin increased, alkaline phosphatase increased, GGT increased) hepatocellular damage, hepatitis, jaundice, hepatomegaly hepatic failure, hepatitis cholestatic, cholestasis, hepatosplenomegaly, liver tenderness, asterixis Skin and subcutaneous tissue disorders Common: Uncommon: Rare:   rash mouth ulceration, alopecia Stevens Johnson syndrome, vesicular rash Musculoskeletal and connective tissue disorders Uncommon:   back pain Renal and urinary disorders Uncommon: Rare:   acute renal failure, renal failure, blood creatinine increased renal tubular acidosis, interstitial nephritis Reproductive system and breast disorders Uncommon: Rare:   menstrual disorder breast pain General disorders and administration site conditions Common: Uncommon: Rare:   pyrexia (fever), asthenia, fatigue oedema, pain, chills, malaise tongue oedema, face oedema Investigations Uncommon:   altered medicine levels Hepatobiliary disorders During post-marketing surveillance severe hepatic injury with fatal outcome has been reported Manufacturer : Schering-Plough Drug Availability : (POM) Drug Updated : 05 November 2010 泊沙康唑(posaconazole)是2006年9月15日由美国FDA批准的一种广谱三唑类抗真菌药,用于难治性疾病或其他药物耐药所引起的真菌感染(如曲霉菌病、结核菌病和镰刀菌病等),该药由美国Scher-ing-Plough公司研制上市,商品名为Noxafil。泊沙康唑是一种新的化学分子实体，是第一个被FDA批准的用于预防由侵袭性曲霉菌引起病变的抗菌药物，属于高亲脂性第二代抗真菌药，与其他唑类抗菌药物相同，该药也是通过与羊毛甾醇14α-脱甲基酶(CYP51或Erg11p)活性部位的血红素辅助因子结合，抑制真菌麦角甾醇的生物合成，破坏细胞膜的形成和完整性而起到抗菌作用。泊沙康唑克服了第一代三唑类药物抗菌谱窄、生物利用度低及耐药性等问题，其抗真菌的作用无论是在体内和体外都已经被证实具有广谱的活性，对念珠菌、各种曲霉菌及其他常见的和非常见的致病真菌均有较大活性。   本药难溶于水，目前只有口服悬液剂，空腹或餐后口服，分别在3~4h和4~10h达到血药峰浓度。血浆蛋白结合率高达98.2%，主要与白蛋白结合。表观分布容积平均高达1744L，具有高度组织穿透力。可透过胎盘屏障，在乳汁中有分泌。   本品适用于多种对两性霉素不能耐受或难治性成人侵袭性真菌感染的治疗；对高危患者预防用药，用于13岁以上、免疫功能低下的患者，特别是患有移植物抗宿主病（graft versus host disease，GVHD）的造血干细胞移植者、白血病患者和由于化疗而长期白细胞减少的患者。本品比对照药物氟康唑和伊曲康唑，能更有效预防侵袭性曲霉菌感染并可降低侵袭性真菌感染相关的病死率。   本品不良反应与其他唑类药物相似，最常见的治疗相关性严重不良反应有胆红素血症、转氨酶升高、肝细胞损害以及恶心和呕吐.