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: ONP 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: ONP

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

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	1551.67	25.69	534	8121	73053	56210359
Death	797.21	25.69	545	8110	340881	55942531
Drug resistance	758.09	25.69	229	8426	20313	56263099
Acquired gene mutation	708.15	25.69	122	8533	765	56282647
Interstitial lung disease	464.76	25.69	209	8446	56854	56226558
Metastases to central nervous system	340.98	25.69	110	8545	12026	56271386
Myelosuppression	275.96	25.69	103	8552	17352	56266060
EGFR gene mutation	252.77	25.69	43	8612	246	56283166
Paronychia	243.47	25.69	69	8586	4849	56278563
Metastases to meninges	169.28	25.69	44	8611	2226	56281186
Malignant transformation	163.20	25.69	31	8624	354	56283058
Hepatic function abnormal	156.34	25.69	85	8570	34473	56248939
Pneumonitis	141.00	25.69	77	8578	31487	56251925
Pleural effusion	126.83	25.69	105	8550	85375	56198037
Metastases to bone	102.35	25.69	53	8602	19455	56263957
Diarrhoea	90.96	25.69	258	8397	638249	55645163
Dermatitis acneiform	88.69	25.69	31	8624	4313	56279099
Platelet count decreased	85.33	25.69	93	8562	106290	56177122
Lung disorder	85.09	25.69	68	8587	52529	56230883
Electrocardiogram QT prolonged	84.97	25.69	69	8586	54519	56228893
Decreased appetite	83.84	25.69	133	8522	219098	56064314
Metastases to liver	83.67	25.69	48	8607	21538	56261874
Cardiac failure	76.93	25.69	78	8577	82015	56201397
Metastases to lung	70.70	25.69	35	8620	11683	56271729
Lymphangiosis carcinomatosa	68.51	25.69	19	8636	1230	56282182
Disease progression	65.93	25.69	81	8574	105092	56178320
Pulmonary embolism	58.44	25.69	77	8578	107047	56176365
Pain	56.76	25.69	16	8639	663168	55620244
Radiation pneumonitis	52.19	25.69	16	8639	1473	56281939
Small cell lung cancer	50.81	25.69	16	8639	1610	56281802
Erythema multiforme	50.22	25.69	26	8629	9528	56273884
Metastasis	46.81	25.69	20	8635	4764	56278648
Carcinoembryonic antigen increased	46.81	25.69	15	8640	1597	56281815
Arthralgia	43.05	25.69	12	8643	501657	55781755
Gene mutation	40.10	25.69	13	8642	1436	56281976
Cardiomyopathy	39.79	25.69	27	8628	16231	56267181
Drug ineffective	37.78	25.69	52	8603	918937	55364475
Dry skin	35.66	25.69	40	8615	47069	56236343
Liver disorder	34.14	25.69	38	8617	44332	56239080
Deep vein thrombosis	33.97	25.69	50	8605	76927	56206485
Multiple-drug resistance	33.63	25.69	15	8640	3959	56279453
Malignant pleural effusion	33.60	25.69	13	8642	2403	56281009
Taste disorder	33.40	25.69	20	8635	9695	56273717
Blood creatine phosphokinase increased	32.63	25.69	30	8625	27922	56255490
Respiratory failure	32.60	25.69	55	8600	95007	56188405
Neutrophil count decreased	32.19	25.69	39	8616	49783	56233629
Joint swelling	31.01	25.69	4	8651	289796	55993616
Ejection fraction decreased	30.67	25.69	25	8630	19816	56263596
Metastases to lymph nodes	30.07	25.69	17	8638	7406	56276006
Rash	29.89	25.69	152	8503	492895	55790517
Skin toxicity	29.88	25.69	14	8641	4139	56279273
Off label use	29.33	25.69	165	8490	556015	55727397
Drug-induced liver injury	29.10	25.69	31	8624	34431	56248981
Thrombocytopenia	28.54	25.69	64	8591	136160	56147252
Bronchial carcinoma	26.64	25.69	8	8647	687	56282725
Pulmonary alveolar haemorrhage	26.50	25.69	13	8642	4251	56279161

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	799.46	30.77	320	3843	78678	31614503
Drug resistance	454.29	30.77	154	4009	23299	31669882
Acquired gene mutation	375.01	30.77	74	4089	1246	31691935
Death	275.33	30.77	282	3881	360287	31332894
Interstitial lung disease	241.28	30.77	130	4033	61273	31631908
EGFR gene mutation	200.37	30.77	31	4132	105	31693076
Metastases to central nervous system	191.03	30.77	61	4102	7575	31685606
Metastases to meninges	130.56	30.77	31	4132	1268	31691913
Pneumonitis	111.97	30.77	62	4101	30590	31662591
Myelosuppression	91.97	30.77	43	4120	14877	31678304
Paronychia	77.50	30.77	25	4138	3193	31689988
Hepatic function abnormal	66.81	30.77	50	4113	41172	31652009
Malignant transformation	58.88	30.77	15	4148	822	31692359
Metastases to bone	53.93	30.77	27	4136	10821	31682360
Metastases to lung	47.96	30.77	23	4140	8399	31684782
Metastases to liver	47.10	30.77	26	4137	12701	31680480
Lung disorder	45.34	30.77	36	4127	32276	31660905
Dermatitis acneiform	39.82	30.77	18	4145	5749	31687432
Lymphangiosis carcinomatosa	39.57	30.77	11	4152	843	31692338
Liver disorder	39.34	30.77	32	4131	29675	31663506
Radiation pneumonitis	39.20	30.77	14	4149	2430	31690751
Pulmonary embolism	37.89	30.77	50	4113	81596	31611585
Decreased appetite	36.44	30.77	69	4094	153148	31540033
Pleural effusion	34.94	30.77	46	4117	74874	31618307

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	1663.01	24.30	645	10469	121094	70796236
Drug resistance	1085.46	24.30	350	10764	37840	70879490
Acquired gene mutation	931.53	24.30	176	10938	1922	70915408
Interstitial lung disease	657.26	24.30	322	10792	104363	70812967
Death	556.10	24.30	527	10587	509534	70407796
EGFR gene mutation	384.86	24.30	65	11049	346	70916984
Metastases to central nervous system	378.46	24.30	126	10988	14908	70902422
Myelosuppression	340.02	24.30	140	10974	30005	70887325
Paronychia	289.65	24.30	86	11028	6988	70910342
Hepatic function abnormal	214.07	24.30	133	10981	67863	70849467
Malignant transformation	197.31	24.30	44	11070	1129	70916201
Metastases to meninges	186.37	24.30	51	11063	3085	70914245
Pneumonitis	169.78	24.30	106	11008	54491	70862839
Pleural effusion	144.45	24.30	138	10976	132726	70784604
Metastases to bone	131.40	24.30	66	11048	22310	70895020
Lung disorder	130.78	24.30	99	11015	69385	70847945
Dermatitis acneiform	123.11	24.30	48	11066	8897	70908433
Metastases to lung	112.87	24.30	54	11060	16430	70900900
Metastases to liver	111.29	24.30	62	11052	25816	70891514
Lymphangiosis carcinomatosa	108.71	24.30	30	11084	1871	70915459
Decreased appetite	107.38	24.30	180	10934	304600	70612730
Diarrhoea	97.81	24.30	306	10808	783035	70134295
Electrocardiogram QT prolonged	96.89	24.30	90	11024	83427	70833903
Platelet count decreased	95.26	24.30	128	10986	178094	70739236
Radiation pneumonitis	85.13	24.30	29	11085	3664	70913666
Liver disorder	76.56	24.30	69	11045	61499	70855831
Pulmonary embolism	72.85	24.30	105	11009	155762	70761568
Cardiac failure	68.99	24.30	98	11016	143443	70773887
Malignant pleural effusion	62.13	24.30	22	11092	3117	70914213
Rash	62.07	24.30	198	10916	510364	70406966
Small cell lung cancer	60.22	24.30	21	11093	2845	70914485
Erythema multiforme	58.70	24.30	35	11079	16529	70900801
Carcinoembryonic antigen increased	54.98	24.30	18	11096	2012	70915318
Metastases to lymph nodes	53.48	24.30	27	11087	9211	70908119
Taste disorder	48.17	24.30	27	11087	11358	70905972
Multiple-drug resistance	47.03	24.30	23	11091	7332	70909998
Metastasis	44.81	24.30	21	11093	6093	70911237
Pain	43.81	24.30	22	11092	628794	70288536
Arthralgia	42.64	24.30	13	11101	503377	70413953
Drug-induced liver injury	42.33	24.30	48	11066	56065	70861265
Cerebral infarction	41.64	24.30	42	11072	42967	70874363
Dry skin	39.09	24.30	46	11068	55885	70861445
Cardiac dysfunction	38.37	24.30	16	11098	3521	70913809
Gene mutation	37.66	24.30	14	11100	2277	70915053
Pulmonary toxicity	36.14	24.30	22	11092	10776	70906554
Pneumothorax	34.16	24.30	30	11084	25816	70891514
Cardiomyopathy	33.63	24.30	30	11084	26343	70890987
Erythema dyschromicum perstans	31.93	24.30	6	11108	63	70917267
Hypotension	31.52	24.30	12	11102	404369	70512961
Disease progression	31.21	24.30	73	11041	156599	70760731
Bone marrow failure	30.48	24.30	38	11076	48972	70868358
Ejection fraction decreased	29.70	24.30	30	11084	30732	70886598
Metastases to adrenals	29.59	24.30	10	11104	1232	70916098
Drug ineffective	29.41	24.30	65	11049	939687	69977643
Joint swelling	28.99	24.30	3	11111	253208	70664122
HER2 gene amplification	28.81	24.30	4	11110	3	70917327
Respiratory failure	28.70	24.30	74	11040	168661	70748669
Deep vein thrombosis	28.11	24.30	57	11057	110985	70806345
BRAF V600E mutation positive	27.51	24.30	5	11109	43	70917287
Weight increased	27.41	24.30	3	11111	242328	70675002
Thrombocytopenia	26.46	24.30	90	11024	239020	70678310
Metastases to pleura	25.18	24.30	9	11105	1309	70916021
Cardiac failure acute	24.52	24.30	21	11093	17466	70899864
Nasopharyngitis	24.51	24.30	3	11111	222203	70695127

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	Nov. 13, 2022	FOR TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), AS DETECTED BY AN FDA-APPROVED TEST, WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
EQ 80MG BASE	TAGRISSO	ASTRAZENECA	N208065	Nov. 13, 2015	RX	TABLET	ORAL	Nov. 13, 2022	FOR TREATMENT OF PATIENTS WITH METASTATIC EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) T790M MUTATION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC), AS DETECTED BY AN FDA-APPROVED TEST, WHO HAVE PROGRESSED ON OR AFTER EGFR TKI THERAPY
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
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.79	CHEMBL
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
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		IC50	6.75	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	6.28	CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN		IC50	6.04	CHEMBL
Receptor tyrosine-protein kinase erbB-3	Kinase	P21860	ERBB3_HUMAN		IC50	8.68	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	5.53	CHEMBL
Dipeptidyl peptidase 1	Enzyme	P53634	CATC_HUMAN		IC50	4.48	CHEMBL
Cysteine--tRNA ligase, cytoplasmic	Enzyme	P49589	SYCC_HUMAN		Kd	7.92	CHEMBL
Tyrosine-protein kinase Tec	Kinase	P42680	TEC_HUMAN		Kd	6.49	CHEMBL
Epidermal growth factor receptor	Kinase		EGFR_MOUSE		IC50	7.09	CHEMBL

External reference:

ID	Source
3C06JJ0Z2O	UNII
1421373-66-1	SECONDARY_CAS_RN
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
4035124	VANDF

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	0310-1350	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