Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Lorlatinib
Drug ID BADD_D02504
Description Lorlatinib has been used in trials studying the basic science and treatment of Non-small Cell Lung Cancer and anaplastic lymphoma kinase (ALK)-positive Non-Small Cell Lung Cancer (NSCLC) and ROS1-positive NSCLC. Despite initial responses from the use of various ALK inhibitors, however, it is virtually almost guaranteed that all patients with the condition in question will develop tumour progression or resistance to the current therapy in use [A40086]. Considered a third-generation ALK tyrosine kinase inhibitor (TKI) for patients with ALK-positive metastatic NSCLC, lorlatinib's most optimal place in the treatment sequence of this condition has most recently been identified with its latest approval by the US FDA in November of 2018 for the indication of treating those patients' disease which has progressed even after the use of first and second-generation TKIs like crizotinib, alectinib, or ceritinib [L4848, FDA Label]. Loratinib's ability to move past the blood-brain barrier facilitates its ability to treat progressive or worsening brain metastases as well [L4848, A40078].
Indications and Usage Lorlatinib is a third-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) [L4848] indicated for the treatment of patients with ALK-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on a) the prior use of crizotinib and at least one other ALK inhibitor for metastatic disease, or b) the prior use of alectinib as the first ALK inhibitor therapy for metastatic disease, or c) the prior use of certinib as the first ALK inhibitor therapy for metastatic disease [L848, FDA Label].
Marketing Status approved; investigational
ATC Code L01ED05
DrugBank ID DB12130
KEGG ID D11012
MeSH ID C000590786
PubChem ID 71731823
TTD Drug ID D0AF6O
NDC Product Code 53869-1043; 53869-0131; 63539-927; 0069-0231; 0069-0227
UNII OSP71S83EU
Synonyms lorlatinib | loratinib | (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-H)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile | PF-06463922 | PF06463922 | Lorbrena | 7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11)benzoxadiazacyclotetradecine-3-carbonitrile
Chemical Information
Molecular Formula C21H19FN6O2
CAS Registry Number 1454846-35-5
SMILES CC1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Nephrotic syndrome20.05.01.0020.000168%
Nervous system disorder17.02.10.0010.002798%Not Available
Nervousness19.06.02.0030.000246%Not Available
Neuropathy peripheral17.09.03.0030.001198%Not Available
Neurotoxicity17.02.10.002; 12.03.01.0110.000616%Not Available
Night sweats08.01.03.031; 23.02.03.0060.000246%Not Available
Nightmare19.02.03.0030.000604%Not Available
Oedema14.05.06.010; 08.01.07.0060.005462%Not Available
Oedema peripheral02.05.04.007; 14.05.06.011; 08.01.07.0070.003705%
Pain08.01.08.004--
Pancreatitis07.18.01.0010.000224%
Papilloedema24.03.07.001; 17.07.02.004; 06.09.02.0020.000112%
Paranoia19.05.01.0050.000112%Not Available
Pathological fracture16.32.03.007; 15.08.02.008; 12.04.02.0060.000112%Not Available
Pericardial effusion02.06.01.0020.000728%
Personality change19.05.01.006; 17.02.05.0190.000604%
Pleural effusion22.05.02.0020.001589%
Pleurisy22.05.01.0010.000112%Not Available
Pleuritic pain22.12.01.0070.000246%
Pneumonitis22.01.01.0060.001186%
Polyneuropathy17.09.03.0120.000280%Not Available
Proteinuria20.02.01.0110.000112%
Pulmonary congestion22.01.03.002; 02.05.02.002; 24.03.08.0010.000112%Not Available
Pulmonary embolism24.01.06.001; 22.06.02.0010.000895%Not Available
Pulmonary hypertension24.08.03.002; 22.06.01.0010.000168%
Pulmonary oedema22.01.03.003; 02.05.02.0030.000336%
Respiratory arrest22.02.01.0090.000112%Not Available
Respiratory disorder22.02.07.0020.000246%Not Available
Respiratory failure22.02.06.002; 14.01.04.0030.000560%
Retinal detachment12.01.04.004; 06.09.03.0030.000112%
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