LORVIQUA® (lorlatinib) as monotherapy is indicated for the first-line treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC) or for patients with ALK-positive metastatic NSCLC whose disease has progressed after alectinib or ceritinib as the first ALK tyrosine kinase inhibitor (TKI) therapy, or crizotinib and at least one other ALK TKI1
Contraindications and Warnings & Precautions Summary of Safety Profile

Safety Profile

Contraindications

  • LORVIQUA® is contraindicated in patients taking strong CYP3A inducers, due to the potential for serious hepatotoxicity (aspartate aminotransferase [AST] and alanine aminotransferase [ALT] elevations)1​​​​​​​

Warnings & Precautions

Hyperlipidaemia1
  • ​​​​​​​The use of LORVIQUA® has been associated with increases in serum cholesterol and triglycerides. Serum cholesterol and triglycerides should be monitored before initiation of LORVIQUA®; 2, 4 and 8 weeks after initiating LORVIQUA®; and periodically thereafter. Initiation, or increase in the dose, of lipid-lowering agents is required

Central nervous system effects1
  • Central nervous system (CNS) effects have ben observed in patients receiving LORVIQUA® including seizures, psychotic effects, changes in cognitive function, mood (including suicidal ideation), mental status, sleep, and speech
  • Dose modification or discontinuation may be required for those patients who develop CNS effects

Atrioventricular block1
  • PR interval prolongation and atrioventricular (AV) block events have been reported in patients receiving LORVIQUA®. Monitor electrocardiogram (ECG) prior to initiating LORVIQUA® and monthly thereafter, particularly in patients with predisposing conditions to the occurrence of clinically significant cardiac events
  • Dose modification may be required for those patients who develop AV block

Lipase and amylase increase1
  • Elevations of lipase and/or amylase have occurred in patients receiving LORVIQUA®. Median time of occurrence of increase in serum lipase and amylase is 70 days (range: 7 to 696 days) and 41 days (range: 7 to 489 days), respectively. Risk of pancreatitis should be considered in patients receiving LORVIQUA® due to concomitant hypertriglyceridaemia and/or a potential intrinsic mechanism. Patients should be monitored for lipase and amylase elevations prior to the start of LORVIQUA® treatment and regularly thereafter as clinically indicated

Interstitial lung disease/pneumonitis1
  • Severe or life threatening pulmonary adverse drug reactions consistent with interstitial lung disease (ILD)/pneumonitis have occurred with LORVIQUA®. Any patients who presents with worsening of respiratory symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough and fever) should be promptly evaluated for ILD/pneumonitis
  • LORVIQUA® should be withheld and/or permanently discontinued based on severity

Hypertension1
  • Hypertension has been reported in patients receiving LORVIQUA®. Blood pressure should be controlled prior to initiation of LORVIQUA®. Blood pressure should be monitored after 2 weeks and at least monthly thereafter during treatment with LORVIQUA®
  • LORVIQUA® should be withheld and resumed at a reduced dose or permanently discontinued based on severity

Hyperglycaemia1
  • Hyperglycaemia has occurred in patients receiving LORVIQUA®. Fasting serum glucose should be assessed prior to initiation of LORVIQUA® and monitored periodically thereafter.
  • LORVIQUA® should be withheld and resumed at a reduced dose or permanently discontinued based on severity

Drug-drug interactions1
  • In a study conducted in healthy volunteers, the concomitant use of LORVIQUA® and rifampin, a strong CYP3A inducer was associated with increases in ALT and AST with no increase of bilirubin and alkaline phosphatase.
  • LORVIQUA® is contraindicated in patients taking strong CYP3A inducers. Discontinue strong CYP3A inducers for at least 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORVIQUA®

Fertility and pregnancy1
  • Based on animal data and mechanism of action, there is a risk of fetal harm if exposed to LORVIQUA®. Women of childbearing potential should be advised to avoid becoming pregnant while receiving LORVIQUA®. A highly effective non-hormonal method of contraception is required for female patients during treatment with LORVIQUA® because LORVIQUA® can render hormonal contraceptives ineffective. If a hormonal method of contraception is unavoidable, then a condom must be used in combination with the hormonal method. Effective contraception must be continued for at least 21 days after completing therapy
  • ​​​​​​​During treatment with LORVIQUA® and for at least 97 days after the final dose, male patients with female partners of reproductive potential must use effective contraception, including a condom, and male patients with pregnant partners must use condoms. Male fertility may be compromised during treatment with LORVIQUA®. Men should seek advice on effective fertility preservation before treatment
Reference
1.Pfizer. LORVIQUA® (lorlatinib) Prescribing Information, Available from: http://labeling.pfizer.com/ShowLabeling.aspx?id=12540 Accessed 5 January 2022.
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The use of lorlatinib has been associated with increases in serum cholesterol and triglycerides. Serum cholesterol and triglycerides should be monitored before the initiation of lorlatinib; 2, 4, and 8 weeks after initiating lorlatinib, and periodically thereafter. Initiation, or increase in the dose, of lipid-lowering agents is required. Central nervous system (CNS) effects have been observed in patients receiving lorlatinib including seizures, psychotic effects, changes in cognitive function, mood (including suicidal ideation), mental status, sleep, and speech. Dose modification or discontinuation may be required for those patients who develop CNS effects. PR interval prolongation and atrioventricular (AV) block events have been reported in patients receiving lorlatinib. Monitor electrocardiogram (ECG) prior to initiating lorlatinib and monthly thereafter, particularly in patients with predisposing conditions to the occurrence of clinically significant cardiac events. Dose modification may be required for those patients who develop AV block. Elevations of lipase and/or amylase have occurred in patients receiving lorlatinib. Median time of occurrence of increase in serum lipase and amylase is 70 days (range: 7 days to 696 days) and 41 days (range: 7 days to 489 days), respectively. Risk of pancreatitis should be considered in patients receiving lorlatinib due to concomitant hypertriglyceridemia and/or a potential intrinsic mechanism. Patients should be monitored for lipase and amylase elevations prior to the start of lorlatinib treatment and regularly thereafter as clinically indicated. Severe or life threatening pulmonary adverse drug reactions consistent with ILD/pneumonitis have occurred with lorlatinib. Any patient who presents with worsening of respiratory symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough and fever) should be promptly evaluated for ILD/pneumonitis. Lorlatinib should be withheld and/or permanently discontinued based on severity. Hypertension has been reported in patients receiving lorlatinib. Blood pressure should be controlled prior to the initiation of lorlatinib. Blood pressure should be monitored after 2 weeks and at least monthly thereafter during treatment with lorlatinib. Lorlatinib should be withheld and resumed at a reduced dose or permanently discontinued based on severity. Hyperglycemia has occurred in patients receiving lorlatinib. Fasting serum glucose should be assessed prior to the initiation of lorlatinib and monitored periodically thereafter. Lorlatinib should be withheld and resumed at a reduced dose or permanently discontinued based on severity. Concomitant use of any strong CYP3A inducer is contraindicated. Any strong CYP3A inducers have to be discontinued for at least 3 plasma half-lives of the strong CYP3A inducer before lorlatinib treatment is started. No clinically meaningful changes in liver function tests were seen in healthy subjects after receiving a combination of lorlatinib with the moderate CYP3A inducer modafinil. Women of childbearing potential should be advised to avoid getting pregnant while receiving lorlatinib. Male fertility may be compromised during treatment with lorlatinib. Men should seek advice on effective fertility preservation before treatment.

​​​​​​​LORVIQUA® Efficacy

​​​​​​​LORVIQUA
® Safety Profile
LORVIQUA® Dosing and Therapy
​​​​​​​Management
Click here for LORVIQUA® Prescribing Information

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