Monday 21 May 2012

Gemcitabine 38mg / ml powder for solution for infusion





1. Name Of The Medicinal Product



Gemcitabine 38mg/ml powder for solution for infusion


2. Qualitative And Quantitative Composition



One ml of the reconstituted solution for infusion (see section 6.6) contains 38mg gemcitabine (as hydrochloride).



200 mg vial:



Each vial contains 200mg of gemcitabine (as hydrochloride).



Contains approximately 0.15mmol (3.56mg) sodium per 200mg vial.



1 g vial:



Each vial contains 1g of gemcitabine (as hydrochloride).



Contains approximately 0.77mmol (17.81mg) sodium per 1g vial.



2 g vial:



Each vial contains 2g of gemcitabine (as hydrochloride).



Contains approximately 1.54mmol (35.62mg) sodium per 2g vial.



For a full list of excipients, see section 6.1.



3. Pharmaceutical Form



Powder for solution for infusion.



White or almost white compact aggregate. After reconstitution in sodium chloride 0.9% the solution is clear to pale opalescent and colourless to pale yellow.



The pH of the reconstituted solution in sodium chloride 0.9% solution is 3.0 ± 0.3.



The osmolarity of the reconstituted solution (38mg/ml of gemcitabine (as hydrochloride) in sodium chloride 0.9% solution) is 775 mOsm/l.



4. Clinical Particulars



4.1 Therapeutic Indications



Gemcitabine is indicated for the treatment of locally advanced or metastatic bladder cancer in combination with cisplatin.



Gemcitabine is indicated for treatment of patients with locally advanced or metastatic adenocarcinoma of the pancreas.



Gemcitabine, in combination with cisplatin is indicated as first line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC). Gemcitabine monotherapy can be considered in elderly patients or those with performance status 2.



Gemcitabine is indicated for the treatment of patients with locally advanced or metastatic epithelial ovarian carcinoma, in combination with carboplatin, in patients with relapsed disease following a recurrence-free interval of at least 6 months after platinum-based, first-line therapy.



Gemcitabine, in combination with paclitaxel, is indicated for the treatment of patients with unresectable, locally recurrent or metastatic breast cancer who have relapsed following adjuvant/neoadjuvant chemotherapy. Prior chemotherapy should have included an anthracycline unless clinically contraindicated.



4.2 Posology And Method Of Administration



Gemcitabine should only be prescribed by a physician qualified in the use of anti-cancer chemotherapy.



Recommended posology



Bladder cancer



Combination use



The recommended dose for gemcitabine is 1000mg/m2, given by 302 on Day 1 following gemcitabine or day 2 of each 28



Pancreatic cancer



The recommended dose of gemcitabine is 1000mg/m2, given by 30



Non small cell lung cancer



Monotherapy



The recommended dose of gemcitabine is 1000mg/m2, given by 30



Combination use



The recommended dose for gemcitabine is 1250mg/m2 body surface area given as a 30



Cisplatin has been used at doses between 75-100mg/m2 once every 3 weeks.



Breast cancer



Combination use



Gemcitabine in combination with paclitaxel is recommended using paclitaxel (175mg/m2) administered on Day 1 over approximately 32) as a 306/l) prior to initiation of gemcitabine + paclitaxel combination.



Ovarian cancer



Combination use



Gemcitabine in combination with carboplatin is recommended using gemcitabine 1000mg/m2 administered on Days 1 and 8 of each 21



Monitoring for toxicity and dose modification due to toxicity



Dose modification due to non haematological toxicity



Periodic physical examination and checks of renal and hepatic function should be made to detect non-haematological toxicity. Dosage reduction with each cycle or within a cycle may be applied based upon the grade of toxicity experienced by the patient. In general, for severe (Grade 3 or 4) non-haematological toxicity, except nausea/vomiting, therapy with gemcitabine should be withheld or decreased depending on the judgement of the treating physician. Doses should be withheld until toxicity has resolved in the opinion of the physician.



For cisplatin, carboplatin, and paclitaxel dosage adjustment in combination therapy, please refer to the corresponding Summary of Product Characteristics.



Dose modification due to haematological toxicity



Initiation of a cycle



For all indications, the patient must be monitored before each dose for platelet and granulocyte counts. Patients should have an absolute granulocyte count of at least 1,500 (x 106/l) and platelet account of 100,000 (x 106/l) prior to the initiation of a cycle.



Within a cycle



Dose modifications of gemcitabine within a cycle should be performed according to the following tables:



















Dose modification of gemcitabine within a cycle for bladder cancer, NSCLC and pancreatic cancer, given in monotherapy or in combination with cisplatin


  


Absolute granulocyte count



(x 106/l)




Platelet count



(x 106/l)




Percentage of standard dose of gemcitabine (%)




> 1,000                                                and




> 100,000




100




500-1,000                                            or




50,000-100,000




75




<500                                                    or




< 50,000




Omit dose *



*Treatment omitted will not be re-instated within a cycle before the absolute granulocyte count reaches at least 500 (x106/l) and the platelet count reaches 50,000 (x106/l).






















Dose modification of gemcitabine within a cycle for breast cancer, given in combination with paclitaxel


  


Absolute granulocyte count



(x 106/l)




Platelet count



(x 106/l)




Percentage of standard dose of gemcitabine (%)







>75,000




100




1,000- <1,200                                      or




50,000-75,000




75




700- <1,000                                         and







50




<700                                                   or




<50,000




Omit dose*



*Treatment omitted will not be re-instated within a cycle. Treatment will start on day 1 of the next cycle once the absolute granulocyte count reaches at least 1,500 (x106/l) and the platelet count reaches 100,000 (x106/l).



















Dose modification of gemcitabine within a cycle for ovarian cancer, given in combination with carboplatin


  


Absolute granulocyte count



(x 106/l)




Platelet count



(x 106/l)




Percentage of standard dose of gemcitabine (%)




> 1,500                                                and







100




1000-1,500                                          or




75,000-100,000




50




<1000                                                  or




< 75,000




Omit dose*



*Treatment omitted will not be re-instated within a cycle. Treatment will start on day 1 of the next cycle once the absolute granulocyte count reaches at least 1,500 (x106/l) and the platelet count reaches 100,000 (x106/l).



Dose modifications due to haematological toxicity in subsequent cycles, for all indications



The gemcitabine dose should be reduced to 75% of the original cycle initiation dose, in the case of the following haematological toxicities:



• Absolute granulocyte count < 500 x 106/l for more than 5 days



• Absolute granulocyte count < 100 x 106/l for more than 3 days



• Febrile neutropaenia



• Platelets < 25,000 x 106/l



• Cycle delay of more than 1 week due to toxicity



Method of administration



The medicinal product is tolerated well during infusion and may be administered ambulant. If extravasation occurs, generally the infusion must be stopped immediately and started again in another blood vessel. The patient should be monitored carefully after the administration.



For instructions on reconstitution, see section 6.6



Special populations



Patients with renal or hepatic impairment



Gemcitabine should be used with caution in patients with hepatic or renal insufficiency as there is insufficient information from clinical studies to allow for clear dose recommendations for these patient populations (see sections 4.4 and 5.2).



Elderly population(> 65 years)



Gemcitabine has been well tolerated in patients over the age of 65. There is no evidence to suggest that dose adjustments, other than those already recommended for all patients, are necessary in the elderly (see section 5.2).



Paediatric population (< 18 years)



Gemcitabine is not recommended for use in children under 18 years of age due to insufficient data on safety and efficacy.



4.3 Contraindications



Hypersensitivity to the active substance or to any of the excipients.



Breast-feeding (see section 4.6).



4.4 Special Warnings And Precautions For Use



Prolongation of the infusion time and increased dosing frequency have been shown to increase toxicity.



Haematological toxicity



Gemcitabine can suppress bone marrow function as manifested by leucopaenia, thrombocytopaenia and anaemia.



Patients receiving gemcitabine should be monitored prior to each dose for platelet, leucocyte and granulocyte counts. Suspension or modification of therapy should be considered when drug-induced bone marrow depression is detected (see section 4.2). However, myelosuppression is short lived and usually does not result in dose reduction and rarely in discontinuation.



Peripheral blood counts may continue to deteriorate after gemcitabine administration has been stopped. In patients with impaired bone marrow function, the treatment should be started with caution. As with other cytotoxic treatments, the risk of cumulative bone-marrow suppression must be considered when gemcitabine treatment is given together with other chemotherapy.



Hepatic insufficiency



Administration of gemcitabine in patients with concurrent liver metastases or a pre-existing medical history of hepatitis, alcoholism or liver cirrhosis may lead to exacerbation of the underlying hepatic insufficiency.



Laboratory evaluation of renal and hepatic function (including virological tests) should be performed periodically.



Gemcitabine should be used with caution in patients with hepatic insufficiency or with impaired renal function as there is insufficient information from clinical studies to allow clear dose recommendation for this patient population (see section 4.2).



Concomitant radiotherapy



Concomitant radiotherapy (given together or



Live vaccinations



Yellow fever vaccine and other live attenuated vaccines are not recommended in patients treated with gemcitabine (see section 4.5).



Cardiovascular



Due to the risk of cardiac and/or vascular disorders with gemcitabine, particular caution must be exercised with patients presenting a history of cardiovascular events.



Pulmonary



Pulmonary effects, sometimes severe (such as pulmonary oedema, interstitial pneumonitis or adult respiratory distress syndrome (ARDS)) have been reported in association with gemcitabine therapy. The aetiology of these effects is unknown. If such effects develop, consideration should be made to discontinuing gemcitabine therapy. Early use of supportive care measure may help ameliorate the condition.



Renal



Clinical findings consistent with the haemolytic uraemic syndrome (HUS) were rarely reported in patients receiving gemcitabine (see section 4.8). Gemcitabine should be discontinued at the first signs of any evidence of microangiopathic haemolytic anaemia, such as rapidly falling haemoglobin with concomitant thrombocytopaenia, elevation of serum bilirubin, serum creatinine, blood urea nitrogen, or LDH. Renal failure may not be reversible with discontinuation of therapy and dialysis may be required.



Fertility



In fertility studies gemcitabine caused hypospermatogenesis in male mice (see section 5.3). Therefore, men being treated with gemcitabine are advised not to father a child during and up to 6 months after treatment and to seek further advice regarding cryoconservation of sperm prior to treatment because of the possibility of infertility due to therapy with gemcitabine (see section 4.6).



Sodium



Vial of 200mg gemcitabine contains 3.56mg (<1mmol) sodium.



Vial of 1g gemcitabine contains 17.81mg (< 1mmol) sodium.



Vial of 2g gemcitabine contains 35.62mg (1.54mmol) sodium.



This should be taken into consideration by patients on a controlled sodium diet.



4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction



No specific interaction studies have been performed (see section 5.2)



Radiotherapy



Concurrent (given together or 2 was administered concurrently for up to 6 consecutive weeks with therapeutic thoracic radiation to patients with non-small cell lung cancer, significant toxicity in the form of severe, and potentially life threatening mucositis, especially oesophagitis, and pneumonitis was observed, particularly in patients receiving large volumes of radiotherapy [median treatment volumes 4,795 cm3]. Studies done subsequently have suggested that it is feasible to administer gemcitabine at lower doses with concurrent radiotherapy with predictable toxicity, such as a phase II study in non-small cell lung cancer, where thoracic radiation doses of 66 Gy were applied concomitantly with an administration with gemcitabine (600mg/m2, four times) and cisplatin (80mg/m2 twice) during 6 weeks. The optimum regimen for safe administration of gemcitabine with therapeutic doses of radiation has not yet been determined in all tumour types.



Non-concurrent (given>7 days apart)- Analysis of the data does not indicate any enhanced toxicity when gemcitabine is administered more than 7 days before or after radiation, other than radiation recall. Data suggest that gemcitabine can be started after the acute effects of radiation have resolved or at least one week after radiation.



Radiation injury has been reported on targeted tissues (e.g. oesophagitis, colitis, and pneumonitis) in association with both concurrent and non-concurrent use of gemcitabine.



Others



Yellow fever and other live attenuated vaccines are not recommended due to the risk of systemic, possibly fatal, disease, particularly in immunosuppressed patients.



4.6 Pregnancy And Lactation



Pregnancy



There are no adequate data from the use of gemcitabine in pregnant women. Studies in animals have shown reproductive toxicity (see section 5.3). Based on results from animal studies and the mechanism of action of gemcitabine, this substance should not be used during pregnancy unless clearly necessary. Women should be advised not to become pregnant during treatment with gemcitabine and to warn their attending physician immediately, should this occur after all.



Breast-feeding



It is not known whether gemcitabine is excreted in human milk and adverse effects on the suckling child cannot be excluded. Breast-feeding must be discontinued during gemcitabine therapy.



Fertility



In fertility studies gemcitabine caused hypospermatogenesis in male mice (see section 5.3). Therefore, men being treated with gemcitabine are advised not to father a child during and up to 6 months after treatment and to seek further advice regarding cryoconservation of sperm prior to treatment because of the possibility of infertility due to therapy with gemcitabine.



4.7 Effects On Ability To Drive And Use Machines



No studies on the effects on the ability to drive and use machines have been performed. However, gemcitabine has been reported to cause mild to moderate somnolence, especially in combination with alcohol consumption. Patients should be cautioned against driving or operating machinery until it is established that they do not become somnolent.



4.8 Undesirable Effects



The most commonly reported adverse drug reactions associated with gemcitabine treatment include: nausea with or without vomiting, raised liver transaminases (AST/ALT) and alkaline phosphatase, reported in approximately 60% of patients; proteinuria and haematuria reported in approximately 50% patients; dyspnoea reported in 10



The frequency and severity of the adverse reactions are affected by the dose, infusion rate and intervals between doses (see section 4.4). Dose



Clinical trial data



Frequencies are defined as: Very common (



The following table of undesirable effects and frequencies is based on data from clinical trials. Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.


































System Organ Class




Frequency grouping




Blood and lymphatic system disorders




Very common



• Leucopaenia (Neutropaenia Grade 3 = 19.3 %; Grade 4 = 6 %).



Bone-marrow suppression is usually mild to moderate and mostly affects the granulocyte count (see section 4.2)



• Thrombocytopaenia



• Anaemia



Common



• Febrile neutropaenia



Very rare



• Thrombocytosis




Immune system disorders




Very Rare



• Anaphylactoid reaction




Metabolism and nutrition disorders




Common



• Anorexia




Nervous system disorders




Common



• Headache



• Insomnia



• Somnolence




Cardiac disorders




Rare



• Myocardial infarct




Vascular disorders




Rare



• Hypotension




Respiratory, thoracic and mediastinal disorders




Very common



• Dyspnoea –usually mild and passes rapidly without treatment



Common



• Cough



• Rhinitis



Uncommon



• Interstitial pneumonitis (see section 4.4)



• Bronchospasm –usually mild and transient but may require parenteral treatment




Gastrointestinal disorders




Very common



• Vomiting



• Nausea



Common



• Diarrhoea



• Stomatitis and ulceration of the mouth



• Constipation




Hepatobiliary disorders




Very common



• Elevation of liver transaminases (AST and ALT) and alkaline phosphatase



Common



• Increased bilirubin



Rare



• Increased gamma-glutamyl transferase (GGT)




Skin and subcutaneous tissue disorders




Very common



• Allergic skin rash frequently associated with pruritus



• Alopecia



Common



• Itching



•Sweating



Rare



• Ulceration



• Vesicle and sore formation



• Scaling



Very rare



• Severe skin reactions, including desquamation and bullous skin eruptions




Musculoskeletal and connective tissue disorders




Common



• Back pain



• Myalgia




Renal and urinary disorders




Very Common



• Haematuria



• Mild proteinuria




General disorders and administration site conditions




Very common



• Influenza-like symptoms - the most common symptoms are fever, headache, chills, myalgia, asthenia and anorexia. Cough, rhinitis, malaise, perspiration and sleeping difficulties have also been reported.



• Oedema/peripheral oedema-including facial oedema. Oedema is usually reversible after stopping treatment



Common



• Fever



• Asthenia



• Chills



Rare



• Injection site reactions-mainly mild in nature




Injury, poisoning, and procedural Complications




Radiation toxicity (see section 4.5).



Postmarketing experience (spontaneous reports) frequency not known (can't be estimated from the available data)



Nervous system disorders



Cerebrovascular accident



Cardiac disorders



Arrythmias, predominantly supraventricular in nature



Heart failure



Vascular disorders



Clinical signs of peripheral vasculitis and gangrene



Respiratory, thoracic and mediastinal disorders



Pulmonary oedema



Adult respiratory distress syndrome (see section 4.4)



Gastrointestinal disorders



Ischaemic colitis



Hepatobiliary disorders



Serious hepatotoxicity, including liver failure and death



Skin and subcutaneous tissue disorders



Severe skin reactions, including desquamation and bullous skin eruptions, Lyell's Syndrome, Steven-Johnson Syndrome



Renal and urinary disorders



Renal failure (see section 4.4)



Haemolytic uraemic syndrome (see section 4.4)



Injury, poisoning and procedural complications



Radiation recall



Combination use in breast cancer



The frequency of grade 3 and 4 haematological toxicities, particularly neutropaenia, increases when gemcitabine is used in combination with paclitaxel. However, the increase in these adverse reactions is not associated with an increased incidence of infections or haemorrhagic events. Fatigue and febrile neutropaenia occur more frequently when gemcitabine is used in combination with paclitaxel. Fatigue, which is not associated with anaemia, usually resolves after the first cycle.










































































Grade 3 and 4 Adverse Events



Paclitaxel versus gemcitabine plus paclitaxel


    

 


Number (%) of Patients


   


Paclitaxel arm



(N=259)




Gemcitabine plus Paclitaxel arm



(N=262)


   


Grade 3




Grade 4




Grade 3




Grade 4


 


Laboratory



 

 

 

 


Anaemia




5 (1.9)




1 (0.4)




15 (5.7)




3 (1.1)




Thrombocytopaenia




0




0




14 (5.3)




1 (0.4)




Neutropaenia




11 (4.2)




17 (6.6)*




82 (31.3)




45 (17.2)*




Non-laboratory



 

 

 

 


Febrile neutropaenia




3 (1.2)




0




12 (4.6)




1(0.4)




Fatigue




3 (1.2)




1 (0.4)




15 (5.7)




2 (0.8)




Diarrhoea




5 (1.9)




0




8 (3.1)




0




Motor neuropathy




2(0.8)




0




6(2.3)




1(0.4)




Sensory neuropathy




9(3.5)




0




14(5.3)




1(0.4)



*Grade 4 neutropaenia lasting for more than 7 days occurred in 12.6% of patients in the combination arm and 5.0% of patients in the paclitaxel arm.



Combination use in bladder cancer
































































Grade 3 and 4 Adverse Events



MVAC versus Gemcitabine plus cisplatin


    

 


Number (%) of Patients


   


MVAC (methotrexate, vinblastine, doxorubicin and cisplatin) arm



(N=196)




Gemcitabine plus cisplatin arm



(N=200)


   


Grade 3




Grade 4




Grade 3




Grade 4


 


Laboratory



 

 

 

 


Anaemia




30(16)




4(2)




47(24)




7(4)




Thrombocytopaenia




15(8)




25(13)




57(29)




57(29)




Non-laboratory



 

 

 

 


Nausea and vomiting




37(19)




3(2)




44(22)




0(0)




Diarrhoea




15(8)




1(1)




6(3)




0(0)




Infection




19(10)




10(5)




4(2)




1(1)




Stomatitis




34(18)




8(4)




2(1)




0(0)



Combination use in ovarian cancer

















































Grade 3 and 4 Adverse Events



Carboplatin versus Gemcitabine plus carboplatin


    

 


Number (%) of Patients


   


Carboplatin arm



(N=174)




Gemcitabine plus carboplatin arm



(N=175)


   


Grade 3




Grade 4




Grade 3




Grade 4


 


Laboratory



 

 

 

 


Anaemia




10(5.7)




4(2.3)




39(22.3)




9(5.1)




Neutropaenia




19(10.9)




2(1.1)




73(41.7)




50(28.6)




Thrombocytopaenia




18(10.3)




2(1.1)




53(30.3)




8(4.6)




Leucopaenia




11(6.3)




1(0.6)




84(48.0)




9(5.1)


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