ArticleClinical pharmacokinetics2024
Evaluation of the Effect of Lorlatinib on CYP2B6, CYP2C9, UGT, and P-Glycoprotein Substrates in Patients with Advanced Non-Small Cell Lung Cancer.
Article in Clinical pharmacokinetics, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT01970865 (PHASE 1/2 STUDY OF PF-06463922), which is not on this map. Cited by 5 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Phase 1/2 study of pf-06463922 (an alk/ros1 tyrosine kinase inhibitor) in patients with advanced non-small cell lung cancer harboring specific molecular alterations
Who cites it
5 citing papers in PubMed, 6 citations in OpenAlex.
- Development and Validation of a UPLC-MS/MS for Determination of Loureirin D in Rat Plasma and Its Application to Pharmacokinetics.Biomedical chromatography : BMC · 2026Article
- Long-Term Safety and Management of Adverse Events Associated With Lorlatinib inJournal of the advanced practitioner in oncology · 2025Article
- Refining Criteria for Choosing the First-Line Treatment for Real-World Patients with AdvancedInternational journal of molecular sciences · 2025Review
- Cyp3a4-Mediated in vitro Metabolism and in vivo Disposition of Lorlatinib in Rats.Drug design, development and therapy · 2025Article
- A Pharmacokinetic Study of the Interaction Between Regorafenib and Paracetamol in Male Rats.Pharmaceutics · 2024Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
17 authors at 10 institutions in 5 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectiveLorlatinib is a tyrosine kinase inhibitor approved for the treatment of advanced anaplastic lymphoma kinase-positive non-small cell lung cancer. This study assessed the effect of steady-state lorlatinib on the metabolic enzymes cytochrome P450 (CYP) 2B6, CYP2C9, and uridine 5'-diphospho-glucuronosyltransferase (UGT) and the P-glycoprotein (P-gp) transporter.
methodsThirty-two patients received a single oral dose of a probe drug on Day - 2 to determine the pharmacokinetics of the probe drug alone. Starting on Day 1, patients received 100 mg oral lorlatinib daily. On Day 15, a single oral dose of the probe drug was administered concurrently with lorlatinib. Pharmacokinetic parameters for these probe substrates were assessed.
resultsPlasma exposures of all probe substrates were reduced by lorlatinib compared with the probe alone. The greatest reduction in area under the plasma concentration-time curve from time zero to infinity (AUC
conclusionsLorlatinib is a net moderate inducer of P-gp and a weak inducer of CYP2B6, CYP2C9, and UGT after steady state is achieved with daily dosing. Medications that are P-gp substrates with a narrow therapeutic window should be avoided in patients taking lorlatinib; no dose modifications are needed with substrates of CYP2B6, CYP2C9, or UGT. CLINICALTRIALS: gov: NCT01970865.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.