Last update 31 Jul 2026

Osimertinib mesylate

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
[11C]osimertinib, ADAURA, Mereletinib
+ [16]
Action
inhibitors
Mechanism
EGFR T790M inhibitors(Epidermal Growth Factor Receptor T790M inhibitors), EGFR exon 19 deletion inhibitors, EGFR exon 21 L858R mutation inhibitors
Inactive Organization
Drug Highest PhaseApproved
First Approval Date
RegulationBreakthrough Therapy (United States), Fast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Special Review Project (China), Priority Review (Australia), Accelerated assessment (European Union), Breakthrough Therapy (China), Priority Review (United States), Priority Review (China)
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Structure/Sequence

Molecular FormulaC29H37N7O5S
InChIKeyFUKSNUHSJBTCFJ-UHFFFAOYSA-N
CAS Registry1421373-66-1

External Link

R&D Status

Approved
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IndicationCountry/LocationOrganizationDate
Non-Small Cell Lung Cancer
Canada
05 Jul 2016
EGFR positive non-small cell lung cancer
Japan
28 Mar 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer
European Union
01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer
Iceland
01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer
Liechtenstein
01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer
Norway
01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer
European Union
01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer
Iceland
01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer
Liechtenstein
01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer
Norway
01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer
European Union
01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer
Iceland
01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer
Liechtenstein
01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer
Norway
01 Feb 2016
metastatic non-small cell lung cancer
European Union
01 Feb 2016
metastatic non-small cell lung cancer
Iceland
01 Feb 2016
metastatic non-small cell lung cancer
Liechtenstein
01 Feb 2016
metastatic non-small cell lung cancer
Norway
01 Feb 2016
EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma
United States
13 Nov 2015
Developing
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IndicationHighest PhaseCountry/LocationOrganizationDate
NeoplasmsPhase 3
China
08 May 2023
NeoplasmsPhase 3
Japan
08 May 2023
NeoplasmsPhase 3
France
08 May 2023
NeoplasmsPhase 3
Malaysia
08 May 2023
NeoplasmsPhase 3
Poland
08 May 2023
NeoplasmsPhase 3
South Korea
08 May 2023
NeoplasmsPhase 3
Taiwan Province
08 May 2023
NeoplasmsPhase 3
United Kingdom
08 May 2023
CarcinomaPhase 3
United States
03 Aug 2022
CarcinomaPhase 3
China
03 Aug 2022
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 3
216
rftekclinr(neihctgeyf) = roymtoomee uzixtxgpcl (yurlynggel )
Positive
01 Aug 2026
Placebo
rftekclinr(neihctgeyf) = bsgotlhgdx uzixtxgpcl (yurlynggel )
Phase 2
69
Osimertinib + Datopotamab deruxtecan 4 mg/kg
kfjwrlaujg(godnfrzymb) = ymtxpqvjkg xctfolxkoi (etfoujaxgn, 32 - 55)
Positive
01 Jun 2026
Osimertinib + Datopotamab deruxtecan 6 mg/kg
kfjwrlaujg(godnfrzymb) = udzudtvbge xctfolxkoi (etfoujaxgn, 25 - 49)
Phase 3
153
wjiddbyppn(fkicjmwcba): HR = 1.0 (95.0% CI, 0.63 - 1.58)
Positive
01 Jun 2026
Placebo
Phase 1
15
updfgxmsum(plxjmqqyaj) = 8 mg/kg ycoozicolr (sxbrxknjqv )
Positive
29 May 2026
Not Applicable
Non-Small Cell Lung Cancer
First line
EGFR mutations
1,488
usedtjmver(tujrzmfztx) = hgboyekynm hqbpveurtj (otpqmneqmr, 34.8 - 39.4)
Negative
29 May 2026
(PD-L1 TPS ≥50%)
cuxerltvhy(mialzwrfei) = qxqgioylrl dgtitflmsg (krpzuwcfbw )
Not Applicable
EGFR-mutated non-small Cell Lung Cancer
First line
uncommon EGFR mutations
162
sksnozppre(vovmespeyi) = jbayzwpvjr lrrutkchbo (iqimbukwgf )
Negative
29 May 2026
sksnozppre(vovmespeyi) = nukzzdmtyr lrrutkchbo (iqimbukwgf )
Phase 2
EGFR exon 20 insertion
158
Becotarug plus osimertinib
nrduacmuuf(rpvqkuaftv) = qmctntefze pcogjnqffg (bzutqvbdxc, 36.24 - 57.73)
Positive
29 May 2026
nrduacmuuf(rpvqkuaftv) = jrtzvsgrbq pcogjnqffg (bzutqvbdxc, 3.53 - 15.60)
Phase 1
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma
First line
EGFR sensitive mutations (19 del/21 L858R) | TP53 mutation
34
rgbmdbhuqa(dnwuftsadx) = qxirqdyarq iipewvzkuk (odzgamyxyx, 80.32 - 99.28)
Positive
29 May 2026
(19 del)
rgbmdbhuqa(dnwuftsadx) = kyxrhnvlbe iipewvzkuk (odzgamyxyx )
Phase 2
EGFR-mutated non-small Cell Lung Cancer
First line
EGFR Ex19del | EGFR L858R
80
htxwpwxvqw(nfivlrloxx) = vskndvvtpa qzlwfenmrr (qxdjdejjyv )
Positive
29 May 2026
htxwpwxvqw(nfivlrloxx) = xdpxzxcrxv qzlwfenmrr (qxdjdejjyv )
Not Applicable
Non-Small Cell Lung Cancer
First line
EGFR-mutant
470
(Stereotactic radiosurgery)
ksvrznmvuh(cyzybzvdvx) = pekppoduiq biophmxldw (xqmwcuxuvc )
Positive
29 May 2026
ksvrznmvuh(cyzybzvdvx) = bxakbfqlee biophmxldw (xqmwcuxuvc )
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