Lorlatinib
Generic Name: lorlatinib
Brand Names:
Lorbrena
11 DESCRIPTION LORBRENA (lorlatinib) is a kinase inhibitor for oral administration. The molecular formula is C 21 H 19 FN 6 O 2 (anhydrous form) and the molecular weight is 406.41 Daltons. The chemical name is (10 R )-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2 H -4,8-methenopyrazolo[4,3- h ][2,5,11] benzoxadiazacyclotetradecine-3-carbonitrile. The chemical structure is shown below: Lorlatinib is a white to off-white powder with a pKa of 4.92.
Overview
11 DESCRIPTION LORBRENA (lorlatinib) is a kinase inhibitor for oral administration. The molecular formula is C 21 H 19 FN 6 O 2 (anhydrous form) and the molecular weight is 406.41 Daltons. The chemical name is (10 R )-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2 H -4,8-methenopyrazolo[4,3- h ][2,5,11] benzoxadiazacyclotetradecine-3-carbonitrile. The chemical structure is shown below: Lorlatinib is a white to off-white powder with a pKa of 4.92.
Uses
1 INDICATIONS AND USAGE LORBRENA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. LORBRENA is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )
Dosage
2 DOSAGE AND ADMINISTRATION Recommended dosage : 100 mg orally once daily. ( 2.2 ) Severe Hepatic Impairment : 50 mg orally once daily. ( 2.5 , 8.6 , 12.3 ) Renal Impairment : 75 mg orally once daily. ( 2.6 , 8.7 , 12.3 ) 2.1 Patient Selection Select patients for the treatment of metastatic NSCLC with LORBRENA based on the presence of ALK positivity in tumor specimens [see Indications and Usage (1) and Clinical Studies (14) ] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics . 2.2 Recommended Dosage The recommended dosage of LORBRENA is 100 mg orally once daily, with or without food, until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3) ] . Swallow tablets whole.
Side Effects
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers [see Warnings and Precautions (5.1) ] • Central Nervous System Effects [see Warnings and Precautions (5.2) ] • Hyperlipidemia [see Warnings and Precautions (5.3) ] • Atrioventricular Block [see Warnings and Precautions (5.4) ] • Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.5) ] • Hypertension [see Warnings and Precautions (5.6) ] • Hyperglycemia [see Warnings and Precautions (5.7) ] Most common (incidence ≥20%) adverse reactions and Grade 3–4 laboratory abnormalities are edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hyperchole...
Interactions
7 DRUG INTERACTIONS • Strong CYP3A Inducers : Contraindicated. ( 2.4 , 7.1 ) • Moderate CYP3A Inducers : Avoid concomitant use. If concomitant use cannot be avoided, increase the LORBRENA dose. ( 2.4 , 7.1 ) • Strong CYP3A Inhibitors : Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. ( 2.4 , 7.1 ) • Fluconazole : Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. ( 2.4 , 7.1 ) • Certain CYP3A Substrates : Avoid concomitant use with CYP3A substrates for which minimal concentration changes may lead to serious therapeutic failures. ( 7.2 ) • Certain P-gp Substrates : Avoid concomitant use with P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures.
Warnings
5 WARNINGS AND PRECAUTIONS • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers : Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA. ( 2.4 , 5.1 ) • Central Nervous System (CNS) Effects : CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity. ( 2.3 , 5.2 ) • Hyperlipidemia : Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity. 4 CONTRAINDICATIONS LORBRENA is contraindicated in patients taking strong CYP3A inducers, due to the potential for serious hepatotoxicity [see Warnings and Precautions (5.1) ] . Concomitant use with strong CYP3A inducers. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of 100 mg once daily based on AUC (see Data ) .
Storage
Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
Frequently Asked Questions
What is Lorlatinib used for?▼
1 INDICATIONS AND USAGE LORBRENA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. LORBRENA is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )
What are the side effects of Lorlatinib?▼
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers [see Warnings and Precautions (5.1) ] • Central Nervous System Effects [see Warnings and Precautions (5.2) ] • Hyperlipidemia [see Warnings and Precautions (5.3) ] • Atrioventricular Block [see Warnings and Precautions (5.4) ] • Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.5) ] • Hypertension [see Warnings and Precautions (5.6) ] • Hyperglycemia [see Warnings and Precautions (5.7) ] Most common (incidence ≥20%) adverse reactions and Grade 3–4 laboratory abnormalities are edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hyperchole...
Can I take Lorlatinib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of 100 mg once daily based on AUC (see Data ) .
What are the important warnings for Lorlatinib?▼
5 WARNINGS AND PRECAUTIONS • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers : Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA. ( 2.4 , 5.1 ) • Central Nervous System (CNS) Effects : CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity. ( 2.3 , 5.2 ) • Hyperlipidemia : Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity. 4 CONTRAINDICATIONS LORBRENA is contraindicated in patients taking strong CYP3A inducers, due to the potential for serious hepatotoxicity [see Warnings and Precautions (5.1) ] . Concomitant use with strong CYP3A inducers. ( 4 )
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11 DESCRIPTION Lotilaner is a member of the isoxazoline family of compounds. Its chemical name is 2-Thiophenecarboxamide, 5-[(5S)-4,5-dihydro-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-3-isoxazolyl]-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-2-thiophenecarboxamide. The molecular formula is C 20 H 14 Cl 3 F 6 N 3 O 3 S. The molecular weight is 596.76 g/mol.
Breathing Air
breathing air
Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.