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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5062	1421373-65-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: osimertinib tagrisso AZD9291 AZD-9291 AZD 9291 osimertinib mesylate osimertinib mesilate AZD9291 mesylate mereletinib	Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. In cultured cells and animal tumor implantation models, osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications. Molecular weight: 499.62 Formula: C28H33N7O2 CLOGP: 4.60 LIPINSKI: 0 HAC: 9 HDO: 2 TPSA: 87.55 ALOGS: -4.35 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

osimertinib
tagrisso
AZD9291
AZD-9291
AZD 9291
osimertinib mesylate
osimertinib mesilate
AZD9291 mesylate
mereletinib

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. In cultured cells and animal tumor implantation models, osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications.

Molecular weight: 499.62
Formula: C28H33N7O2
CLOGP: 4.60
LIPINSKI: 0
HAC: 9
HDO: 2
TPSA: 87.55
ALOGS: -4.35
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
80	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company
Feb. 2, 2016	EMA	AstraZeneca AB
Nov. 13, 2015	FDA	ASTRAZENECA PHARMS
March 28, 2016	PMDA	AstraZeneca K.K.

FDA Adverse Event Reporting System (Female)

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
Malignant neoplasm progression	1852.38	24.51	637	9771	81484	63397130
Death	1269.06	24.51	772	9636	373609	63105005
Drug resistance	904.13	24.51	273	10135	22660	63455954
Acquired gene mutation	815.28	24.51	141	10267	842	63477772
Interstitial lung disease	497.12	24.51	229	10179	61679	63416935
Myelosuppression	473.77	24.51	169	10239	23534	63455080
Metastases to central nervous system	402.19	24.51	129	10279	12976	63465638
EGFR gene mutation	303.84	24.51	51	10357	246	63478368
Paronychia	261.30	24.51	76	10332	5489	63473125
Metastases to meninges	217.71	24.51	56	10352	2546	63476068
Malignant transformation	202.32	24.51	38	10370	379	63478235
Hepatic function abnormal	158.83	24.51	90	10318	37052	63441562
Pneumonitis	149.67	24.51	85	10323	35137	63443477
Pleural effusion	139.00	24.51	118	10290	93092	63385522
Metastases to bone	112.18	24.51	59	10349	20960	63457654
Diarrhoea	104.55	24.51	304	10104	715062	62763552
Electrocardiogram QT prolonged	92.03	24.51	77	10331	59453	63419161
Platelet count decreased	91.98	24.51	104	10304	116018	63362596
Dermatitis acneiform	89.84	24.51	33	10375	4963	63473651
Decreased appetite	88.34	24.51	152	10256	250900	63227714
Disease progression	85.64	24.51	103	10305	122655	63355959
Metastases to liver	84.42	24.51	51	10357	23588	63455026
Metastases to lung	80.23	24.51	40	10368	12710	63465904
Lung disorder	77.10	24.51	71	10337	62190	63416424
Cardiac failure	76.00	24.51	83	10325	89059	63389555
Lymphangiosis carcinomatosa	73.44	24.51	21	10387	1424	63477190
Pain	64.05	24.51	21	10387	740607	62738007
Small cell lung cancer	62.09	24.51	19	10389	1630	63476984
Pulmonary embolism	58.14	24.51	83	10325	116601	63362013
Gene mutation	57.69	24.51	18	10390	1647	63476967
Radiation pneumonitis	54.37	24.51	17	10391	1566	63477048
Arthralgia	53.13	24.51	14	10394	569696	62908918
Carcinoembryonic antigen increased	52.55	24.51	17	10391	1748	63476866
Blood creatine phosphokinase increased	52.54	24.51	42	10366	30388	63448226
Metastasis	50.40	24.51	22	10386	5175	63473439
Ejection fraction decreased	50	24.51	36	10372	22296	63456318
Erythema multiforme	49.89	24.51	27	10381	10142	63468472
Cardiomyopathy	45.56	24.51	31	10377	17553	63461061
Drug ineffective	40.05	24.51	69	10339	1044696	62433918
Joint swelling	39.45	24.51	4	10404	327662	63150952
Dry skin	36.80	24.51	46	10362	56841	63421773
Deep vein thrombosis	36.52	24.51	56	10352	83744	63394870
Skin toxicity	36.33	24.51	17	10391	4697	63473917
Thrombocytopenia	35.21	24.51	77	10331	151080	63327534
Drug-induced liver injury	35.20	24.51	38	10370	40184	63438430
Multiple-drug resistance	34.84	24.51	17	10391	5153	63473461
Headache	33.23	24.51	33	10375	633208	62845406
Malignant pleural effusion	31.84	24.51	13	10395	2593	63476021
Rash	31.22	24.51	177	10231	560694	62917920
Respiratory failure	31.00	24.51	58	10350	101800	63376814
Nasopharyngitis	30.86	24.51	3	10405	254254	63224360
Metastases to lymph nodes	30.15	24.51	18	10390	8140	63470474
Bone marrow failure	29.80	24.51	30	10378	29260	63449354
Abdominal discomfort	29.63	24.51	8	10400	320877	63157737
Infusion related reaction	29.53	24.51	3	10405	245518	63233096
Off label use	29.50	24.51	200	10208	674262	62804352
Neutrophil count decreased	29.36	24.51	41	10367	56365	63422249
Cardiac failure acute	27.58	24.51	18	10390	9505	63469109
Pulmonary alveolar haemorrhage	27.47	24.51	14	10394	4654	63473960
Weight increased	27.09	24.51	5	10403	260787	63217827
Hepatitis	27.06	24.51	33	10375	39755	63438859
Cardiotoxicity	27.04	24.51	17	10391	8421	63470193
Liver disorder	26.43	24.51	38	10370	53649	63424965
Neoplasm progression	26.06	24.51	31	10377	36397	63442217
Taste disorder	26.04	24.51	20	10388	13642	63464972
Skin disorder	26.03	24.51	28	10380	29479	63449135
Bronchial carcinoma	25.33	24.51	8	10400	761	63477853
Pneumothorax	25.03	24.51	21	10387	16240	63462374

FDA Adverse Event Reporting System (Male)

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
Malignant neoplasm progression	909.34	27.05	369	4546	87677	34864339
Drug resistance	481.95	27.05	168	4747	25759	34926257
Death	467.42	27.05	406	4509	397643	34554373
Acquired gene mutation	404.05	27.05	80	4835	1275	34950741
Interstitial lung disease	252.40	27.05	140	4775	65142	34886874
Metastases to central nervous system	227.30	27.05	72	4843	8133	34943883
EGFR gene mutation	204.40	27.05	33	4882	144	34951872
Myelosuppression	151.08	27.05	67	4848	19198	34932818
Metastases to meninges	150.49	27.05	36	4879	1418	34950598
Pneumonitis	102.20	27.05	62	4853	33816	34918200
Paronychia	86.48	27.05	28	4887	3377	34948639
Hepatic function abnormal	82.36	27.05	60	4855	44303	34907713
Malignant transformation	77.44	27.05	19	4896	832	34951184
Metastases to bone	69.99	27.05	34	4881	11936	34940080
Metastases to liver	57.22	27.05	31	4884	13632	34938384
Metastases to lung	53.05	27.05	26	4889	9294	34942722
Lung disorder	47.07	27.05	39	4876	34657	34917359
Dermatitis acneiform	46.77	27.05	21	4894	6168	34945848
Pleural effusion	41.33	27.05	54	4861	81492	34870524
Decreased appetite	40.85	27.05	79	4836	166313	34785703
Liver disorder	40.46	27.05	35	4880	32962	34919054
Lymphangiosis carcinomatosa	37.88	27.05	11	4904	921	34951095
Radiation pneumonitis	37.21	27.05	14	4901	2626	34949390
Pulmonary embolism	33.00	27.05	51	4864	89695	34862321
Metastases to adrenals	32.68	27.05	10	4905	1002	34951014
Metastases to lymph nodes	32.43	27.05	15	4900	4713	34947303
Rash	31.48	27.05	85	4830	222667	34729349
Disease progression	31.11	27.05	55	4860	108022	34843994
Electrocardiogram QT prolonged	28.71	27.05	32	4883	40920	34911096
Metastasis	27.97	27.05	13	4902	4131	34947885

FDA Adverse Event Reporting System (Geriatric)

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
Malignant neoplasm progression	1944.68	22.77	755	12370	135235	79596028
Drug resistance	1275.08	22.77	410	12715	41803	79689460
Acquired gene mutation	1061.75	22.77	200	12925	2033	79729230
Death	862.38	22.77	721	12404	565793	79165470
Interstitial lung disease	701.20	22.77	350	12775	112250	79619013
Myelosuppression	587.04	22.77	228	12897	40068	79691195
EGFR gene mutation	448.92	22.77	76	13049	388	79730875
Metastases to central nervous system	432.34	22.77	144	12981	16231	79715032
Paronychia	311.10	22.77	94	13031	7714	79723549
Malignant transformation	248.50	22.77	54	13071	1164	79730099
Hepatic function abnormal	238.68	22.77	149	12976	72958	79658305
Metastases to meninges	217.77	22.77	60	13065	3541	79727722
Pneumonitis	168.81	22.77	112	13013	60748	79670515
Pleural effusion	163.06	22.77	157	12968	145105	79586158
Metastases to bone	154.56	22.77	77	13048	24350	79706913
Dermatitis acneiform	132.80	22.77	53	13072	9940	79721323
Metastases to lung	132.15	22.77	63	13062	18100	79713163
Metastases to liver	129.94	22.77	72	13053	28242	79703021
Lung disorder	121.72	22.77	103	13022	80454	79650809
Lymphangiosis carcinomatosa	117	22.77	33	13092	2121	79729142
Decreased appetite	114.33	22.77	203	12922	342215	79389048
Diarrhoea	112.44	22.77	358	12767	880131	78851132
Platelet count decreased	107.97	22.77	146	12979	194518	79536745
Electrocardiogram QT prolonged	107.61	22.77	101	13024	90285	79640978
Radiation pneumonitis	85.76	22.77	30	13095	3903	79727360
Cardiac failure	75.16	22.77	109	13016	154733	79576530
Small cell lung cancer	74.63	22.77	25	13100	2855	79728408
Pulmonary embolism	70.78	22.77	112	13013	171542	79559721
Liver disorder	69.55	22.77	72	13053	72345	79658918
Rash	66.14	22.77	227	12898	578131	79153132
Carcinoembryonic antigen increased	64.56	22.77	21	13104	2188	79729075
Gene mutation	64.42	22.77	22	13103	2664	79728599
Metastases to lymph nodes	60.54	22.77	31	13094	10366	79720897
Malignant pleural effusion	59.48	22.77	22	13103	3358	79727905
Erythema multiforme	57.56	22.77	36	13089	17615	79713648
Ejection fraction decreased	51.74	22.77	44	13081	34533	79696730
Multiple-drug resistance	50.53	22.77	26	13099	8782	79722481
Metastasis	50.44	22.77	24	13101	6856	79724407
Arthralgia	50.00	22.77	16	13109	571787	79159476
Pain	49.82	22.77	27	13098	703775	79027488
Drug-induced liver injury	48.35	22.77	57	13068	66060	79665203
Disease progression	45.08	22.77	96	13029	184266	79546997
Cerebral infarction	43.09	22.77	45	13080	45631	79685632
Pulmonary toxicity	41.25	22.77	26	13099	12888	79718375
BRAF V600E mutation positive	39.69	22.77	7	13118	47	79731216
Dry skin	39.13	22.77	52	13073	67943	79663320
Taste disorder	38.77	22.77	27	13098	15796	79715467
Thrombocytopenia	36.41	22.77	111	13014	265148	79466115
Joint swelling	36.30	22.77	3	13122	288643	79442620
Cardiomyopathy	35.83	22.77	33	13092	28741	79702522
Blood creatine phosphokinase increased	35.68	22.77	49	13076	66041	79665222
Cardiac dysfunction	35.25	22.77	16	13109	4108	79727155
Weight increased	34.56	22.77	3	13122	277383	79453880
Metastases to pleura	34.44	22.77	12	13113	1542	79729721
Pneumothorax	34.33	22.77	32	13093	28291	79702972
Hypotension	33.97	22.77	15	13110	440302	79290961
Bone marrow failure	32.39	22.77	41	13084	51066	79680197
Metastases to adrenals	32.31	22.77	11	13114	1319	79729944
Cardiac failure acute	32.30	22.77	26	13099	18903	79712360
Erythema dyschromicum perstans	31.63	22.77	6	13119	63	79731200
Nasopharyngitis	30.94	22.77	3	13122	253878	79477385
Hepatotoxicity	30.67	22.77	40	13085	51312	79679951
Drug ineffective	29.72	22.77	86	13039	1080827	78650436
Deep vein thrombosis	29.57	22.77	63	13062	120856	79610407
HER2 gene amplification	28.61	22.77	4	13121	3	79731260
Infusion related reaction	27.33	22.77	3	13122	230234	79501029
TP53 gene mutation	27.26	22.77	5	13120	43	79731220
Headache	27.21	22.77	41	13084	653731	79077532
Skin toxicity	27.21	22.77	17	13108	8297	79722966
Respiratory failure	26.98	22.77	78	13047	180833	79550430
Cardiotoxicity	25.66	22.77	19	13106	12220	79719043
Confusional state	24.25	22.77	11	13114	317986	79413277
Neoplasm progression	23.04	22.77	35	13090	51647	79679616

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EB04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA MoA	N0000175082	Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000185506	Cytochrome P450 3A4 Inducers
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000191266	Cytochrome P450 1A2 Inducers
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:74440	EGFR antagonoists

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

Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer, positive for epidermal growth factor receptor expression	indication	426964009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.64	acidic
pKa2	7.93	Basic
pKa3	5.6	Basic
pKa4	1.32	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	9732058	July 25, 2032	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	8946235	Aug. 8, 2032	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	ADJUVANT THERAPY AFTER TUMOR RESECTION IN PATIENTS WITH NON-SMALL CELL LUNG CANCER(NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19DELETIONS OR EXON 21 L858R MUTATIONS
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	10183020	Jan. 2, 2035	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21L858R MUTATIONS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	Dec. 18, 2023	INDICATION OF OSIMERTINIB AS ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	Dec. 18, 2023	INDICATION OF OSIMERTINIB AS ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	April 18, 2025	INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	April 18, 2025	INDICATED FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 40MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	Dec. 18, 2027	FOR ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	Dec. 18, 2027	FOR ADJUVANT THERAPY AFTER TUMOR RESECTION IN ADULT PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS HAVE EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 19 DELETIONS OR EXON 21 L858R MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	INHIBITOR	IC50	7.82	SCIENTIFIC LITERATURE	DRUG LABEL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	5.44	CHEMBL
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		IC50	8.32	CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN		IC50	6.04	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		IC50	6.75	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	6.28	CHEMBL
Tyrosine-protein kinase Tec	Kinase	P42680	TEC_HUMAN		Kd	6.49	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.79	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	5.53	CHEMBL
Lysine-specific histone demethylase 1A	Enzyme	O60341	KDM1A_HUMAN		IC50	5.40	CHEMBL
Dipeptidyl peptidase 1	Enzyme	P53634	CATC_HUMAN		IC50	4.48	CHEMBL
Cysteine--tRNA ligase, cytoplasmic	Enzyme	P49589	SYCC_HUMAN		Kd	7.92	CHEMBL
Receptor tyrosine-protein kinase erbB-3	Kinase	P21860	ERBB3_HUMAN		IC50	8.68	CHEMBL
Epidermal growth factor receptor	Kinase		EGFR_MOUSE		IC50	7.09	CHEMBL

External reference:

ID	Source
3C06JJ0Z2O	UNII
1421373-66-1	SECONDARY_CAS_RN
4035124	VANDF
C4058811	UMLSCUI
CHEBI:90943	CHEBI
YY3	PDB_CHEM_ID
CHEMBL3353410	ChEMBL_ID
71496458	PUBCHEM_CID
DB09330	DRUGBANK_ID
CHEMBL3545063	ChEMBL_ID
10043	INN_ID
C000596361	MESH_SUPPLEMENTAL_RECORD_UI
7719	IUPHAR_LIGAND_ID
1721559	RXNORM
237132	MMSL
31292	MMSL
d08397	MMSL
016583	NDDF
016584	NDDF
716032009	SNOMEDCT_US
734660003	SNOMEDCT_US
781312009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1349	TABLET, FILM COATED	40 mg	ORAL	NDA	28 sections
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1349	TABLET, FILM COATED	40 mg	ORAL	NDA	28 sections
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1349	TABLET, FILM COATED	40 mg	ORAL	NDA	28 sections
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1350	TABLET, FILM COATED	80 mg	ORAL	NDA	28 sections
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1350	TABLET, FILM COATED	80 mg	ORAL	NDA	28 sections
TAGRISSO	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1350	TABLET, FILM COATED	80 mg	ORAL	NDA	28 sections