Lorlatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Lorlatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the PMDA in 2018. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2B6 Inducers and Cytochrome P450 3A Inducers. DrugCentral lists 15 molecular targets, including ALK, ROS1 and LTK. Recorded indications include ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.

• Approval status: onp (first approved 2018 by the PMDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2B6 Inducers; Cytochrome P450 3A Inducers.
• Molecular targets: ALK, ROS1, LTK and FER (15 listed in DrugCentral).
• Indications: ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.
• ATC code: L01ED05 (Anaplastic lymphoma kinase (ALK) inhibitors).
• Molecular formula: C21H19FN6O2; molecular weight 406.42 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• ALK fusion gene-positive non-small-cell lung cancer
• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2B6 Inducers; Cytochrome P450 3A Inducers; Kinase Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Organic Anion Transporter 3 Inhibitors; Organic Cation Transporter 1 Inhibitors; P-Glycoprotein Inducers
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (15)

Target	Gene	Action	Activity
ALK tyrosine kinase receptor	ALK	inhibitor	Ki 9.96
Proto-oncogene tyrosine-protein kinase ROS	ROS1	inhibitor	IC50 9.30
Leukocyte tyrosine kinase receptor	LTK	inhibitor	IC50 8.57
Tyrosine-protein kinase Fer	FER	inhibitor	IC50 8.48
Tyrosine-protein kinase Fes/Fps	FES	inhibitor	IC50 8.22
Protein-tyrosine kinase 2-beta	PTK2B	inhibitor	IC50 7.85
Focal adhesion kinase 1	PTK2	inhibitor	IC50 7.77
Activated CDC42 kinase 1	TNK2	inhibitor	IC50 7.77
BDNF/NT-3 growth factors receptor	NTRK2	inhibitor	IC50 7.64
High affinity nerve growth factor receptor	NTRK1	inhibitor	IC50 7.62
Activin receptor type-1	ACVR1	unknown	IC50 7.54
NT-3 growth factor receptor	NTRK3	inhibitor	IC50 7.34
Tyrosine-protein kinase FRK	FRK	unknown	IC50 7.28
Epidermal growth factor receptor	EGFR	unknown	Ki 7.25
Tyrosine-protein kinase JAK2	JAK2	unknown	Ki 6.28

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2019-06-06	EMA	—	PFIZER EUROPE MA EEIG
2018-09-21	PMDA	—	Pfizer Japan Inc
2018-09-21	FDA	—	PFIZER INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01ED05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ALK · Testing Required
• FDA label: ALK · Testing Required
• FDA label: ROS1 · No Clinical PGx
• HCSC label: ALK · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Neoplasm progression	1430.9
Death	611.3
Hallucination	567.6
Hyperlipidaemia	388.4
Hypertriglyceridaemia	324.3
Hypercholesterolaemia	309.0
Oedema	241.5
Hallucination, auditory	208.0
Cognitive disorder	189.1
Nervous system disorder	168.0
Hallucination, visual	167.9
Blood triglycerides increased	148.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Lorlatinib is on its molecule page.

• Molecular formula: C₂₁H₁₉FN₆O₂
• Molecular weight: 406.42 g/mol
• CAS number: 1454846-35-5
• InChIKey: IIXWYSCJSQVBQM-LLVKDONJSA-N
• PubChem CID: 71731823

C[C@H]1OC2=C(N)N=CC(=C2)C2=C(C#N)N(C)N=C2CN(C)C(=O)C2=CC=C(F)C=C12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lorlatinib used for?

DrugCentral lists the following indications for Lorlatinib: ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.

How does Lorlatinib work?

Lorlatinib is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2B6 Inducers and Cytochrome P450 3A Inducers; its molecular targets in DrugCentral include ALK (inhibitor), ROS1 (inhibitor), LTK (inhibitor) and FER (inhibitor).

When was Lorlatinib first approved?

Lorlatinib was first approved by the PMDA in 2018.

What drug class does Lorlatinib belong to?

Lorlatinib is in the Kinase Inhibitor class.

What is the chemical formula of Lorlatinib?

Lorlatinib has the molecular formula C21H19FN6O2 and a molecular weight of 406.42 g/mol.

Sources

• DrugCentral drug card 5302 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3286830 — compound record and bioactivity
• PubChem CID 71731823 — chemical identifiers
• DrugBank DB12130 — drug record
• FDA UNII OSP71S83EU — substance identity
• DailyMed: FDA labels for Lorlatinib — current prescribing information (label search)
• UniProt Q9UM73 (ALK) — target protein
• UniProt P08922 (ROS1) — target protein
• UniProt P29376 (LTK) — target protein
• UniProt P16591 (FER) — target protein
• UniProt P07332 (FES) — target protein
• UniProt Q14289 (PTK2B) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.