- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Oral formulations of mobocertinib.
Advanced/metastatic non-small cell lung cancer with EGFR exon20ins mutation
Locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutation in adults who have received prior platinum-based chemotherapy.
Recommended dose: 160mg once daily.
Additional Dosage Information
If a dose is missed by more than 6 hours, the patient should not take a dose that day and wait until the next scheduled dose the following day.
If the patient vomits after taking a dose, the dose should not be repeated. The patient should wait until the next scheduled dose the following day.
First dose reduction: 120mg once daily
Second dose reduction: 80mg once daily
Dose modifications for adverse reactions
Grade 2 (QTc interval 481 msec to 500 msec): On first occurrence, withhold treatment until recovery to less than or equal to Grade 1 or baseline. Upon recovery, resume treatment at the same dose. Upon recurrence, withhold treatment until recovery to less than or equal to Grade 1 or baseline. Upon recovery, resume treatment at the next lower dose or permanently discontinue treatment.
Grade 3 (QTc interval greater than or equal to 501 msec or QTc interval greater than 60 msec increase from baseline): On first occurrence, withhold treatment until recovery to less than or equal to Grade 1 or baseline. Upon recovery, resume treatment at the next lower dose or permanently discontinue treatment. Upon recurrence, permanently discontinue treatment.
Grade 4 (Torsade de Pointes, polymorphic ventricular tachycardia, signs/symptoms of serious arrhythmia): Permanently discontinue treatment.
Interstitial lung disease (ILD)/pneumonitis
Any grade: Withhold treatment if ILD/pneumonitis is suspected. Permanently discontinue treatment if ILD/pneumonitis is confirmed.
Decreased ejection fraction or heart failure
Grade 2 decreased ejection fraction: Withhold treatment until recovery to less than or equal to Grade 1 or baseline. If recovery occurs within 2 weeks, resume treatment at the same dose or the next lower dose. If not recovered to baseline within 2 weeks, permanently discontinue treatment.
Greater than or equal to Grade 2 cardiac failure or Grade 3 or 4 decreased ejection fraction: Permanently discontinue treatment.
Grade 1 or 2: At the first onset of diarrhoea, initiate treatment with anti-diarrhoeal. No dose modification required.
Intolerable or recurrent Grade 2 or Grade 3: Withhold treatment until recover to Grade 1 or lower. Upon recovery, resume treatment at the same dose or the next lower dose.
Grade 4: On first occurrence, withhold treatment until recovery to Grade 1 or lower. If recovery occurs within 2 weeks, resume treatment at the next lower dose. If not recovered to Grade 1 or lower within 2 weeks, permanently discontinue treatment. Upon recurrence, permanently discontinue treatment.
Grade 2 (greater than 2 to 5 x ULN and asymptomatic): Continue at the same dose or the next lower dose.
Asymptomatic Grade 3 (greater than 5 x ULN): Withhold treatment until recovery to Grade 1 or lower. If recovery occurs within 2 weeks, resume treatment at the same dose or the next lower dose. If not recovered to Grade 1 or lower within 2 weeks, permanently discontinue treatment.
Symptomatic Grade 3 and Grade 4: Withhold treatment until recovery to Grade 1 or lower. If recovery occurs within 2 weeks, resume treatment at the next lower dose. If not recovered to Grade 1 or lower within 2 weeks, permanently discontinue treatment.
Other non-haematological toxicity
Grade 2: Withhold treatment for intolerable or recurrent Grade 2 toxicity until symptoms resolve. Upon recovery, resume treatment at the same dose or next lower dose.
Grade 3: Withhold treatment until recovery to Grade 1 or lower. Upon recovery, resume treatment at the same dose or the next lower dose.
Grade 4: Consider permanently discontinuing treatment.
Other haematological toxicity
Grade 3: Withhold treatment until recovery to Grade 2 or lower. Upon recovery, resume treatment at the same dose or the next lower dose.
Grade 4: Consider permanently discontinuing treatment.
Dose modifications due to interacting medicines
If concomitant moderate CYP 3A inhibitors cannot be avoided the dose of mobocertinib should be reduced by approximately 50%. After discontinuation of a moderate CYP 3A inhibitor, mobocertinib should be resumed at the previously tolerated dose.
Children under 18 years
Long QT syndrome
Moderate hepatic impairment
Severe renal impairment
Torsade de pointes
Precautions and Warnings
Family history of long QT syndrome
History of treatment with anthracyclines
History of torsade de pointes
Correct electrolyte disorders before treatment
Advise ability to drive/operate machinery may be affected by side effects
Advise patient to have anti-diarrhoeals readily available
Confirm EGFR exon 20 insertion mutation status prior to treatment
Maintain adequate hydration of patient prior / during treatment
Treatment to be initiated and supervised by a specialist
Consult local policy on the safe use of oral anti-cancer drugs
Staff: Not to be handled by pregnant staff
Monitor cardiac function before and periodically during treatment
Perform ECG before and during treatment
Monitor for signs and symptoms of interstitial lung disease
Monitor for signs and symptoms of pneumonitis
Monitor patients for signs and symptoms of cardiac failure
Monitor serum amylase and lipase regularly
Monitor serum electrolytes
Consider discontinuing therapy if significant cardiac failure develops
Predisposition QT prolongation: Counsel patient on symptoms of arrhythmias
Suspend treatment if pneumonitis is suspected
Consider discontinuing therapy if serious cardiac arrhythmias occur
Discontinue if evidence of interstitial lung disease
Discontinue if Grade 3 or 4 LVEF reduction occurs
Discontinue if polymorphic ventricular tachycardia occurs
Discontinue if Torsade de Pointes should occur during treatment
Discontinue if treatment related pneumonitis is diagnosed
Discontinue permanently if QT prolongation and life threatening arrhythmias
Interrupt treatment if QTc interval greater than 480 msec
Permanently discontinue if grade 2 cardiac failure occurs
Permanently discontinue treatment if grade 4 diarrhoea recurs
Permanently discontinue treatment if grade 4 haematological toxicity occurs
Suspend treatment and/or reduce dose in grade 3 non-haematological toxicity
Suspend treatment if grade 3 or greater diarrhoea occurs
Suspend treatment if grade 3 or greater haematological toxicity
Suspend treatment if interstitial lung disease is suspected
Suspend/reduce dose if grade 2 decreased ejection fraction occurs
Suspend/reduce dose if grade 2 or greater elevations in amylase/lipase
Suspend/reduce dose if intolerable/recurrent grade 2 diarrhoea occurs
Suspend/reduce dose if QTc > 500 msec or > 60 msec increase from baseline
Advise patient not to take St John's wort concurrently
Advise patient to avoid grapefruit products
Female:Non-hormonal contraception advised until 1 month after treatment
Male: Contraception required during and for 1 week after treatment
Breastfeeding: Do not breastfeed during & for 1 week after treatment
Patients should have ready access to antidiarrhoeal medicines and should start treatment at the first episode of loose stools or onset of more frequent bowel movements than normal.
Pregnancy and Lactation
Mobocertinib is contraindicated during pregnancy.
The manufacturer states that mobocertinib should not be used during pregnancy unless the clinical condition of the woman requires treatment. There are no data on the use of mobocertinib in pregnant women. However, mobocertinib it is expected to cause foetal harm based on the mechanism of action and data from animal studies which has shown maternal and embryo-foetal toxicity.
Mobocertinib is contraindicated during breastfeeding.
The manufacturer contraindicates breastfeeding during treatment and for 1 week following the final dose. It is unknown whether mobocertinib or its metabolites are excreted in human breast milk.
Alanine aminotransferase increased
Aspartate aminotransferase increased
Elevated amylase levels
Elevated serum lipase
Gastroesophageal reflux disease
Interstitial lung disease
Palmar-Plantar Erythrodysaesthesia syndrome
Prolongation of QT interval
Reduced lymphocyte count
Reduced platelet count
Serum creatinine increased
White blood cell count decreased
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: January 2023
Summary of Product Characteristics: Exkivity 40 mg hard capsules. Takeda UK Ltd. Revised January 2023.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 24 January 2023
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Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.