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Lorbrena (lorlatinib)
Lorbrena works by blocking the activity of the ALK tyrosine kinase receptor, which is a protein that helps cancer cells grow.
Lorbrena (lorlatinib) is a small molecule kinase inhibitor developed by Pfizer, targeting the ALK tyrosine kinase receptor. It is approved for the treatment of ALK fusion gene-positive non-small-cell lung cancer and non-small cell lung cancer. Lorbrena is a patented medication with no generic manufacturers available. Key safety considerations include potential liver damage and increased risk of bleeding. It was FDA-approved in 2018.
At a glance
| Generic name | lorlatinib |
|---|---|
| Sponsor | Pfizer |
| Drug class | Kinase Inhibitor [EPC] |
| Target | ALK tyrosine kinase receptor |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2018 |
Mechanism of action
Lorlatinib is kinase inhibitor with in vitro activity against ALK and ROS1 as well as TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK. Lorlatinib demonstrated in vitro activity against multiple mutant forms of the ALK enzyme, including some mutations detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors.In mice subcutaneously implanted with tumors harboring EML4 fusions with either ALK variant or ALK mutations, including the G1202R and I1171T mutations detected in tumors at the time of disease progression on ALK inhibitors, administration of lorlatinib resulted in antitumor activity. Lorlatinib also demonstrated anti-tumor activity and prolonged survival in mice implanted intracranially with EML4-ALK-driven tumor cell lines. The overall antitumor activity of lorlatinib in in vivo models was dose-dependent and correlated with inhibition of ALK phosphorylation.
Approved indications
- ALK fusion gene-positive non-small-cell lung cancer
- Non-small cell lung cancer
Common side effects
- Edema
- Peripheral neuropathy
- Weight gain
- Cognitive effects
- Fatigue
- Dyspnea
- Arthralgia
- Diarrhea
- Mood effects
- Cough
- Hypercholesterolemia
- Hypertriglyceridemia
Key clinical trials
- Analysis of the Effectiveness and Safety of Lorlatinib in Untreated ALK-Positive NSCLC Patients in a French Real-World Context (NA)
- A Phase 1/2 Study of TRI-611 in ALK-Positive NSCLC (PHASE1,PHASE2)
- Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer (PHASE2)
- Lorlatinib for Newly-Diagnosed High-Grade Glioma With ROS or ALK Fusion (EARLY_PHASE1)
- A Study to Learn About Lorlatinib in Patients With Non-Small Cell Lung Cancer Which Could Not Be Controlled
- Testing the Addition of 131I-MIBG or Lorlatinib to Intensive Therapy in People With High-Risk Neuroblastoma (NBL) (PHASE3)
- Lorlatinib Plus Local Consolidation Therapy In ALK Positive Advanced Non-Small Cell Lung Cancer (PHASE2)
- A Study to Learn About Lorlatinib in Patients With Non-Small Cell Lung Cancer (NSCLC) Which Has Spread Out.
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Lorbrena CI brief — competitive landscape report
- Lorbrena updates RSS · CI watch RSS
- Pfizer portfolio CI