Scroll

lorlatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5302	1454846-35-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lorlatinib lorbrena PF-06463922 PF-6463922 lorviqua	Lorlatinib is a 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. Molecular weight: 406.42 Formula: C21H19FN6O2 CLOGP: 2.07 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 110.06 ALOGS: -3.57 ROTB: 0 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lorlatinib
lorbrena
PF-06463922
PF-6463922
lorviqua

Lorlatinib is a 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.

Molecular weight: 406.42
Formula: C21H19FN6O2
CLOGP: 2.07
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 110.06
ALOGS: -3.57
ROTB: 0

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

Show entries

Search:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.17 mg/mL	Bocci G, Oprea TI, Benet LZ

Showing 1 to 2 of 2 entries

Previous1Next

Approvals:

Show entries

Search:

Date	Agency	Company
June 6, 2019	EMA	PFIZER EUROPE MA EEIG
Sept. 21, 2018	FDA	PFIZER INC
Sept. 21, 2018	PMDA	Pfizer Japan Inc

Showing 1 to 3 of 3 entries

Previous1Next

FDA Adverse Event Reporting System (Female)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neoplasm progression	578.91	31.21	151	2035	36277	63450559
Hypercholesterolaemia	192.50	31.21	57	2129	21277	63465559
Death	172.49	31.21	124	2062	374257	63112579
Hypertriglyceridaemia	159.09	31.21	38	2148	6221	63480615
Hyperlipidaemia	80.96	31.21	29	2157	19542	63467294
Blood triglycerides increased	57.31	31.21	20	2166	12468	63474368
Cognitive disorder	51.80	31.21	29	2157	55786	63431050
Pleural effusion	49.68	31.21	34	2152	93176	63393660
Nervous system disorder	49.38	31.21	20	2166	18746	63468090
Oedema peripheral	48.76	31.21	45	2141	189466	63297370

Showing 1 to 10 of 18 entries

Previous1 2Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neoplasm progression	453.64	33.37	119	1404	23181	34932227
Death	107.77	33.37	107	1416	397942	34557466
Hypercholesterolaemia	101.60	33.37	30	1493	8732	34946676
Hypertriglyceridaemia	44.80	33.37	16	1507	8432	34946976
Oedema peripheral	41.02	33.37	37	1486	119775	34835633
Blood cholesterol increased	34.03	33.37	17	1506	20526	34934882

Showing 1 to 6 of 6 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neoplasm progression	922.31	28.65	246	3192	51436	79689514
Hypercholesterolaemia	264.03	28.65	78	3360	23017	79717933
Death	181.49	28.65	167	3271	566347	79174603
Hypertriglyceridaemia	171.95	28.65	49	3389	12691	79728259
Oedema peripheral	69.85	28.65	69	3369	252219	79488731
Hyperlipidaemia	69.75	28.65	30	3408	26063	79714887
Pleural effusion	60.41	28.65	50	3388	145212	79595738
Hallucination, auditory	59.30	28.65	25	3413	20668	79720282
Oedema	57.89	28.65	45	3393	119535	79621415
Blood cholesterol increased	55.24	28.65	38	3400	83682	79657268

Showing 1 to 10 of 20 entries

Previous1 2Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	L01ED05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62434	ALK inhibitor
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175082	Kinase Inhibitors
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190111	Organic Anion Transporter 3 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers
FDA MoA	N0000191264	P-Glycoprotein Inducers

Showing 1 to 10 of 12 entries

Previous1 2Next

Drug Use | Suggest Off label Use Form| |View source of the data|

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908
ALK fusion gene-positive non-small-cell lung cancer	indication	830151004

Showing 1 to 2 of 2 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.76	Basic

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	10420749	July 27, 2036	TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	10420749	July 27, 2036	TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER, PROGRESSED ON: CRIZOTINIB + AT LEAST 1 OTHER ALK INHIBITOR FOR METASTATIC DISEASE; OR ALECTINIB, OR CERITINIB AS FIRST ALK INHIBITOR FOR METASTATIC DISEASE.
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	10420749	July 27, 2036	TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	10420749	July 27, 2036	TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER, PROGRESSED ON: CRIZOTINIB + AT LEAST 1 OTHER ALK INHIBITOR FOR METASTATIC DISEASE; OR ALECTINIB, OR CERITINIB AS FIRST ALK INHIBITOR FOR METASTATIC DISEASE.

Showing 1 to 4 of 4 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2023	NEW CHEMICAL ENTITY
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	March 3, 2024	EXPANDED INDICATION OF THE TREATMENT OF ADULT PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA-APPROVED TEST
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS PROGRESSED ON ALECTINIB AS THE FIRST ALK INHIBITOR THERAPY FOR METASTATIC DISEASE
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS PROGRESSED ON CERITINIB AS THE FIRST ALK INHIBITOR THERAPY FOR METASTATIC DISEASE
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS PROGRESSED ON CRIZOTINIB AND AT LEAST ONE OTHER ALK INHIBITOR FOR METASTATIC DIESASE
100MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	March 3, 2028	TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST, EXCLUDING PATIENTS WHOSE DISEASE HAS PROGRESSED ON CRIZOTINIB AND AT LEAST ONE OTHER ALK INHIBITOR FOR METASTATIC DISEASE; OR ALECTINIB OR CERITINIB AS THE FIRST ALK INHIBITOR THERAPY FOR METASTATIC DISEASE
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2023	NEW CHEMICAL ENTITY
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	March 3, 2024	EXPANDED INDICATION OF THE TREATMENT OF ADULT PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA-APPROVED TEST
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS PROGRESSED ON ALECTINIB AS THE FIRST ALK INHIBITOR THERAPY FOR METASTATIC DISEASE
25MG	LORBRENA	PFIZER	N210868	Nov. 2, 2018	RX	TABLET	ORAL	Nov. 2, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE DISEASE HAS PROGRESSED ON CERITINIB AS THE FIRST ALK INHIBITOR THERAPY FOR METASTATIC DISEASE

Showing 1 to 10 of 12 entries

Previous1 2Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN	INHIBITOR	IC50	8.22	SCIENTIFIC LITERATURE	DRUG LABEL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN	INHIBITOR	IC50	7.85	SCIENTIFIC LITERATURE	DRUG LABEL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN	INHIBITOR	IC50	7.34	SCIENTIFIC LITERATURE	DRUG LABEL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN	INHIBITOR	IC50	8.57	SCIENTIFIC LITERATURE	DRUG LABEL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	Ki	9.96	SCIENTIFIC LITERATURE	DRUG LABEL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN	INHIBITOR	IC50	9.30	SCIENTIFIC LITERATURE	DRUG LABEL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN	INHIBITOR	IC50	7.77	SCIENTIFIC LITERATURE	DRUG LABEL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN	INHIBITOR	IC50	7.62	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN	INHIBITOR	IC50	8.48	SCIENTIFIC LITERATURE	DRUG LABEL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN	INHIBITOR	IC50	7.77	SCIENTIFIC LITERATURE	DRUG LABEL

Showing 1 to 10 of 14 entries

Previous1 2Next

External reference:

Show entries

Search:

ID	Source
017834	NDDF
10278	INN_ID
2103164	RXNORM
296337	MMSL
35471	MMSL
4037975	VANDF
53P	PDB_CHEM_ID
5P8	PDB_CHEM_ID
71731823	PUBCHEM_CID
7476	IUPHAR_LIGAND_ID

Showing 1 to 10 of 21 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lorbrena	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0227	TABLET, FILM COATED	25 mg	ORAL	NDA	32 sections
Lorbrena	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0231	TABLET, FILM COATED	100 mg	ORAL	NDA	32 sections
Lorbrena	HUMAN PRESCRIPTION DRUG LABEL	1	63539-927	TABLET, FILM COATED	25 mg	ORAL	NDA	31 sections

Showing 1 to 3 of 3 entries

Previous1Next