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)
Psychiatric symptom19.01.02.0010.000112%Not Available
Disease progression08.01.03.0380.001377%
Disease recurrence08.01.03.0500.000246%Not Available
Psychotic disorder19.03.01.0020.000470%
Hyperlipidaemia14.08.03.0010.004533%
Knee deformity15.10.03.0020.000112%Not Available
Renal impairment20.01.03.0100.000728%Not Available
Osteonecrosis of jaw24.04.05.005; 15.02.04.0100.000112%
Pulmonary arterial hypertension24.08.03.003; 22.06.01.0020.000280%Not Available
Neurological decompensation17.02.05.0300.000112%Not Available
Slow speech19.19.02.004; 17.02.08.0160.000224%Not Available
Drug-induced liver injury12.03.01.044; 09.01.07.0230.000728%Not Available
Multiple organ dysfunction syndrome08.01.03.0570.000224%
Anal incontinence17.05.01.021; 07.01.06.0290.000112%
Hallucination, olfactory19.10.04.0050.000168%Not Available
IgA nephropathy20.05.01.016; 10.02.01.0630.000112%Not Available
Persecutory delusion19.10.01.0070.000224%Not Available
Reading disorder19.21.05.0030.000246%Not Available
Disease complication08.01.03.0870.000112%Not Available
Drug effective for unapproved indication12.09.02.001; 08.06.01.0370.000381%Not Available
Gait inability17.02.05.069; 08.01.02.0110.000168%Not Available
Hypersensitivity pneumonitis22.01.01.027; 10.01.03.0560.000112%Not Available
Illness08.01.03.0910.000302%Not Available
Pharyngeal swelling22.04.05.0280.000381%Not Available
Pituitary apoplexy24.07.04.036; 17.08.01.072; 05.03.04.0110.000112%Not Available
Thrombophlebitis migrans24.01.01.043; 16.32.01.0160.000224%Not Available
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