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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:

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

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FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EB04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:74440	EGFR antagonoists
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175082	Kinase Inhibitors
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
MeSH PA	D000970	Antineoplastic Agents

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

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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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

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Orange Book patent data (new drug applications)

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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 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 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	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

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Orange Book exclusivity data (new drug applications)

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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 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 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, 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	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	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

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Bioactivity Summary:

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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

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External reference:

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ID	Source
YY3	PDB_CHEM_ID
016583	NDDF
016584	NDDF
10043	INN_ID
1421373-66-1	SECONDARY_CAS_RN
1721559	RXNORM
237132	MMSL
31292	MMSL
3C06JJ0Z2O	UNII
4035124	VANDF

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Pharmaceutical products:

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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

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