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Orserdu is a brand name for Elacestrant. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: ORSERDU monotherapy is indicated for the treatment of postmenopausal women, and men, with estrogen receptor (ER)-positive, HER2-negative, locally advanced or metastatic breast cancer with an activating ESR1 mutation who have disease progression following at least one line of endocrine therapy including a CDK 4/6…
Verbatim from this product's EMA label. Tap a section to expand.
Treatment with ORSERDU should be initiated by a physician experienced in the use of anticancer therapies. Patients with ER-positive, HER2-negative advanced breast cancer should be selected for treatment with ORSERDU based on the presence of an activating ESR1 mutation in plasma specimens, using a CE marked in vitro diagnostic (IVD) with the corresponding intended purpose.
If the CE-marked IVD 3 is not available, the presence of an activating ESR1 mutation in plasma specimens should be assessed by an alternative validated test. Posology The recommended dose is 345 mg (one 345 mg film-coated tablet), once daily.
The maximum recommended daily dose of ORSERDU is 345 mg. Treatment should continue as long as clinical benefit is observed or until unacceptable toxicity occurs. Missed dose If a dose is missed, it can be taken immediately within 6 hours after the time it is usually taken.
After more than 6 hours, the dose should be skipped for that day. On the next day, ORSERDU should be taken at the usual time. Vomiting If the patient vomits after taking the ORSERDU dose, the patient should not take an additional dose on that day and should resume the usual dosing schedule the next day at the usual time.
8) are provided in Tables 1 and 2: Table 1: ORSERDU dose reduction for adverse reactions ORSERDU dose level Dose and schedule Number and strength of tablets Dose reduction 258 mg once daily Three 86 mg tablets If further dose reduction below 258 mg once daily is required, discontinue ORSERDU.
Table 2:
ORSERDU dose modification guidelines for adverse reactions Severity Dose modification Grade 2 Consider interruption of ORSERDU until recovery to Grade ≤ 1 or baseline. Then resume ORSERDU at the same dose level. Grade 3 Interrupt ORSERDU until recovery to Grade ≤ 1 or baseline.
The dose should be reduced to 258 mg when resuming therapy. If the Grade 3 toxicity recurs, interrupt ORSERDU until recovery to Grade ≤ 1 or baseline. The reduced dose of 258 mg may be resumed at the discretion of the treating physician if the patient is benefiting from treatment.
If a Grade 3 or intolerable adverse reaction recurs, permanently discontinue ORSERDU. Grade 4 Interrupt ORSERDU until recovery to Grade ≤ 1 or baseline. The dose should be reduced to 258 mg when resuming therapy. If a Grade 4 or intolerable adverse reaction recurs, permanently discontinue ORSERDU.
Summary of the safety profile The most common (≥ 10%) adverse reactions with ORSERDU were nausea, triglycerides increased, cholesterol increased, vomiting, fatigue, dyspepsia, diarrhoea, calcium decreased, back pain, creatinine increased, arthralgia, sodium decreased, constipation, headache, hot flush, abdominal pain, anaemia, potassium decreased, and alanine aminotransferase increased.
3%), anaemia (2%), back pain (2%), and bone pain (2%). Serious adverse reactions reported in ≥ 1% of patients included nausea, dyspnoea, and thromboembolism (venous). Adverse reactions leading to discontinuation in ≥ 1% of patients included nausea and decreased appetite.
Adverse reactions leading to dose reduction in ≥ 1% of patients included nausea. 8 Adverse reactions leading to dose interruption in ≥ 1% of patients were nausea, abdominal pain, alanine aminotransferase increased, vomiting, rash, bone pain, decreased appetite, aspartate aminotransferase increased, and diarrhoea.
Tabulated list of adverse reactions Adverse reactions described in the list below reflect exposure to elacestrant in 301 patients with breast cancer in three open label studies (RAD1901-005, RAD1901-106, and RAD1901-308) in which patients received elacestrant 400 mg once daily as a single agent.
The frequencies of adverse reactions are based on all-cause adverse event frequencies identified in patients exposed to elacestrant at the recommended dose in the target indication, whereas frequencies for changes in laboratory parameters are based on worsening from baseline by at least 1 grade and shifts to ≥ grade 3.
The median duration of treatment was 85 days (range 5 to 1288). The adverse reaction frequencies from clinical trials are based on all-cause adverse event frequencies, where a proportion of the events for an adverse reaction may have other causes than the drug, such as the disease, other medication or unrelated causes.
Hepatic impairment ORSERDU is metabolised by the liver, and impaired hepatic function can increase the risk for adverse reactions. Therefore, ORSERDU should be used cautiously in patients with hepatic impairment and patients should be regularly and closely monitored for adverse reactions.
2). 2). Concomitant use with CYP3A4 inhibitors Concomitant administration of ORSERDU with strong CYP3A4 inhibitors including, but not limited to: clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, saquinavir, telaprevir, telithromycin, voriconazole, and grapefruit or grapefruit juice should be avoided.
An alternative concomitant medicinal product with no or minimal potential to inhibit CYP3A4 should be considered. 5). Concomitant administration of ORSERDU with moderate CYP3A4 inhibitors including, but not limited to: aprepitant, ciprofloxacin, conivaptan, crizotinib, cyclosporine, diltiazem, dronedarone, erythromycin, fluconazole, fluvoxamine, grapefruit juice, imatinib, isavuconazole, tofisopam and verapamil should be avoided.
An alternative concomitant medicinal product with no or minimal potential to inhibit CYP3A4 should be considered. 5). Concomitant use with CYP3A4 inducers Concomitant administration of ORSERDU with strong CYP3A4 inducers including, but not limited to: phenytoin, rifampicin, carbamazepine and St John’s Wort (Hypericum perforatum) should be avoided.
An alternative concomitant medicinal product with no or minimal potential to induce CYP3A4 should be considered. 5). Concomitant administration of ORSERDU with moderate CYP3A4 inducers including, but not limited to: bosentan, cenobamate, dabrafenib, efavirenz, etravirine, lorlatinib, phenobarbital, primidone and sotorasib should be avoided.
An alternative concomitant medicinal product with no or minimal potential to induce CYP3A4 should be considered. 5). 8). This should be taken into consideration when prescribing ORSERDU to patients at risk.
1. 5
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Use of ORSERDU with CYP3A4 inhibitors Concomitant use of strong or moderate CYP3A4 inhibitors should be avoided and an alternative concomitant medicinal product with no or minimal potential to inhibit CYP3A4 should be considered. If a strong CYP3A4 inhibitor must be used, the elacestrant dose should be reduced to 86 mg once daily with careful monitoring of tolerability.
If a moderate CYP3A4 inhibitor must be used, the elacestrant dose should be reduced to 172 mg once daily with careful monitoring of tolerability. 4 Subsequent dose reduction to 86 mg once daily may be considered with moderate CYP3A4 inhibitors based on tolerability.
2). 5). Use of ORSERDU with CYP3A4 inducers Concomitant use of strong or moderate CYP3A4 inducers should be avoided and an alternative concomitant medicinal product with no or minimal potential to induce CYP3A4 should be considered. e.
e. treatment periods ≤ 3 days separated by at least 2 weeks or 1 week + 5 half-lives of the CYP3A4 inducer, whichever is longer), continue elacestrant without increasing the dose. 2). Special populations Elderly No dose adjustment is required on the basis of patient age.
2). Hepatic impairment No dose adjustment is recommended for patients with mild hepatic impairment (Child-Pugh A). In patients with moderate hepatic impairment (Child-Pugh B), ORSERDU dose should be reduced to 258 mg. 4). Renal impairment No dose adjustment in subjects with renal impairment is necessary.
2). Paediatric population The safety and efficacy of ORSERDU in children from birth to 18 years of age has not been established. No data are available. Method of administration ORSERDU is for oral use. The tablets should be swallowed whole.
They should not be chewed, crushed or split prior to swallowing. Patients should take their dose of ORSERDU at approximately the same time each day. ORSERDU should be administered with a light meal. 2).
The following convention is used for the classification of the frequency of an adverse drug reaction (ADR) and is based on the Council for International Organizations of Medical Sciences (CIOMS) guidelines: 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 (cannot be estimated from the available data).
Table 3. Adverse reactions in patients treated with elacestrant monotherapy 345 mg in metastatic breast cancer Elacestrant N= 301 Infections and infestations Common Urinary tract infection Blood and lymphatic system disorders Very common Anaemia Common Lymphocyte count decreased Metabolism and nutrition disorders Very common Decreased appetite Psychiatric disorders Common Insomnia Nervous system disorder Very common Headache Common Dizziness, Syncope Vascular disorders Very common Hot flush* Uncommon Thromboembolism (venous)* Respiratory, thoracic and mediastinal disorders Common Dyspnoea, Cough* Gastrointestinal disorders Very common Nausea, Vomiting, Diarrhoea, Constipation, Abdominal pain*, Dyspepsia* Common Stomatitis Hepatobiliary disorders Uncommon Acute hepatic failure Skin and subcutaneous tissue disorders Common Rash* Musculoskeletal and connective tissues disorders Very common Arthralgia, Back pain Common Pain in extremity, Musculoskeletal chest pain *, Bone pain General disorders and administration site conditions Very common Fatigue Common Asthenia 9 Elacestrant N= 301 Investigations Very common Aspartate aminotransferase increased, Triglycerides increased, Cholesterol increased, Alanine aminotransferase increased, Calcium decreased, Creatinine increased, Sodium decreased, Potassium decreased Common Blood alkaline phosphatase increased *Incidence represents a grouping of similar terms.
ADRs listed by system organ class and by decreasing frequency.. Description of selected adverse reactions Nausea Nausea was reported in 35% of patients. 5% of patients. Nausea was generally reported early, with a median time to the first onset 14 days (range: 1 to 490 days).
, over time). 8%) received an antiemetic for the treatment of nausea during the on-treatment period. Elderly In the RAD1901-308 study, 104 patients who received elacestrant were ≥ 65 years and 40 patients were ≥ 75 years. Gastrointestinal disorders were reported more frequently in patients aged ≥ 75 years.
Monitoring of treatment emergent adverse reactions by the treating physician, should include consideration of the patient’s age and comorbidities, when selecting personalised interventions. Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important.
It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system listed in Appendix V.