Drug · Small Molecule

Selumetinib

CI-DRUG-00000548Explore in graph →NCIt C66939 CHEMBL1614701 CIViC Approved

Regulatory

Approvals (10)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory10 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as KOSELUGO (DIN 02530139) under ATC L01EE04 SELUMETINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jan 3, 2023	health-canada-dpd
CA Health Canada	—	Marketed in Canada as KOSELUGO (DIN 02530147) under ATC L01EE04 SELUMETINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jan 3, 2023	health-canada-dpd
CA Health Canada	—	Marketed in Canada as KOSELUGO GRANULES (DIN 02569736) under ATC L01EE04 SELUMETINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approved	—	health-canada-dpd

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 18 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 3	32	8	7	115	10	CA, EU, US	Apr 10, 2020	2006-07
Malignant Lung Neoplasm	Phase3	Phase 3	3	0	1	23	0	—	—	2006-08
Malignant Breast Neoplasm	Phase2	Phase 2	3	1	0	10	0	—	—	Dec 14, 2007
Malignant Ovarian Neoplasm	Phase2	Phase 2	2	1	0	3	0	—

Curated evidence

Clinical evidence (85)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 85 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
FLT3 ITD + FLT3 TKD MUTATION + KRAS Exon 2-3 Mutation + NRAS EXON 2-3 MUTATION + PTPN11 MutationFLT3 NRAS

Clinical trials

Trials with this intervention (116)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 51–100 of 116 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT01783197	Study of Selumetinib in Patients With Previously Treated or Untreated Advanced/Metastatic NSCLC	completed	Phase 1	39	Canadian Cancer Trials GroupNETWORK	1	Aug 4, 2023	clinicaltrials
NCT03745989	Study of MK-8353 + Selumetinib in Advanced/Metastatic Solid Tumors (MK-8353-014)	completed	Phase 1

Molecule

Record

Kind: Small Molecule
Mechanism: Dual specificity mitogen-activated protein kinase kinase 1 inhibitor; Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
Targets: 2 genes
UNII: 6UH91I579U
Aliases: ARRAY142886, ARRY-142886, ARRY-886, AZD 6244, AZD-6244, AZD6244, AZD-6244 HYDROGEN SULFATE, AZD-6244 HYD-SULFATE, AZD6244 (SELUMETINIB), KOSELUGO, KOSELUGO GRANULES, MEK Inhibitor AZD6244, Selumetinib, SELUMETINIB (AZD6244), Selumetinib Sulfate, SELUMETINIB SULFATE

Data updated 21 hours agoSource updated unknown

Identifiers

Codes (10)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EE04	SELUMETINIB
DIN (Health Canada)	02530139

BRAF V600E3
Selumetinib	Childhood Pilocytic Astrocytoma	Predictive	B	Supports Sensitivity Response	3	submitted	EID7485 In a phase 2 trial, patients with pediatric low-grade glioma after at least one standard therapy were treated with MEK1/2 inhibitor selumetinib. In stratum 1, nine patients with WHO grade I pilocytic… (full text at CIViC) PMID 31151904 · Fangusaro et al., 2019 · Open in CIViC	civic
〃	High-Grade Glioma, NOS	Predictive	B	Supports Sensitivity Response	—	submitted	EID2145 In a study of pediatric low-grade gliomas, BRAF V600E mutation was associated with a strong trend toward reduced progression free survival (HR:2.39, 95%CI:0.93-6.15, P=0.07, multivariate analysis). PMID 22492957 · Horbinski et al., 2012 · Open in CIViC	civic
〃	High-Grade Glioma, NOS	Predictive	D	Supports Sensitivity Response	—	submitted	EID2144 In a mouse xenograft model, tumors derived from pilocytic astrocytoma cells that expressed BRAF V600E experienced a complete response to treatment with selumetinib, whereas tumors derived from a wildt… (full text at CIViC) PMID 20806365 · Kolb et al., 2010 · Open in CIViC	civic

BRAF Fusion2
Selumetinib	Childhood Pilocytic Astrocytoma	Predictive	B	Supports Sensitivity Response	3	submitted	EID7486 In a phase 2 trial, patients with pediatric low-grade glioma after at least one standard therapy were treated with MEK1/2 inhibitor selumetinib. In stratum 1, nine patients with WHO grade I pilocytic… (full text at CIViC) PMID 31151904 · Fangusaro et al., 2019 · Open in CIViC	civic
〃	Childhood Pilocytic Astrocytoma	Predictive	D	Supports Sensitivity Response	2	accepted	EID8943 In this preclinical experiment, a pediatric pilocytic astrocytoma cell line (DKFZ-BT66) harboring KIAA1549:BRAF fusion was generated from a two year old patient. Treatment with selumetinib resulted in… (full text at CIViC) PMID 28002790 · Selt et al., 2017 · Open in CIViC	civic

NRAS Q61K3
Selumetinib	Cutaneous MelanomaALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID1475 Preclinical study in melanoma cell lines. NRAS Q61K, in addition to the BRAF V600E mutation was associated with resistance to vemurafenib but sensitivity to AZD6244 (selumetinib) in vitro in the acqui… (full text at CIViC) PMID 22194965 · Atefi et al., 2011 · Open in CIViC	civic
Selumetinib + TrametinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	accepted	EID2907 Of the 4,562 patients with lung cancers, 30 showed NRAS mutations, which corresponded to 9 different amino acid substitutions. Cell lines were developed for 6 of these mutations (one harboring Q61L, t… (full text at CIViC) PMID 23515407 · Ohashi et al., 2013 · Open in CIViC	civic
Dactolisib + SelumetinibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID2192 In 28 out of 40 (70%) metastatic colorectal cancer tumors harboring mutations in KRAS, NRAS, BRAF, or PIK3CA and implanted into mice, the therapeutic combination of the MEK inhibitor AZD6244 and the P… (full text at CIViC) PMID 22392911 · Migliardi et al., 2012 · Open in CIViC	civic

KRAS G12D2
Dactolisib + SelumetinibCombination	Lung Adenocarcinoma	Predictive	D	Supports Sensitivity Response	4	accepted	EID305 The use of NVP-BEZ235 in conjunction with ARRY-142886, but not as monotherapy, in a lung cancer mouse model with an inducible KRAS G12D mutation (lox-stop-lox KRAS G12D floxed via inhaled adenoviral C… (full text at CIViC) PMID 19029981 · Engelman et al., 2008 · Open in CIViC	civic
Dactolisib + SelumetinibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID2218 In 28 out of 40 (70%) metastatic colorectal cancer tumors harboring KRAS, NRAS, BRAF or PIK3CA mutations and implanted into mice, the therapeutic combination of the MEK inhibitor AZD6244 and the PI3K/… (full text at CIViC) PMID 22392911 · Migliardi et al., 2012 · Open in CIViC	civic

KRAS G12C3
Docetaxel + SelumetinibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	2	accepted	EID1142 83 patients from a phase II trial (docetaxel + placebo or MEK1/2 inhibitor selumetinib) with KRAS mutant tumors were retrospectively assessed for differences in OS, PFS, ORR and change in tumor size a… (full text at CIViC) PMID 26125448 · Jänne et al., 2015 · Open in CIViC	civic
Selumetinib + TizaterkibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID9146 In preclinical experiments using the KRAS G12C mutant NSCLC cell line NCI-H358, combination AZD0364 and selumetinib treatment showed synergistic effect as defined by a Loewe score >=5, as well as stro… (full text at CIViC) PMID 33273059 · Flemington et al., 2021 · Open in CIViC	civic
Dactolisib + SelumetinibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	accepted	EID2212 In 28 out of 40 (70%) metastatic colorectal cancer tumors harboring BRAF, KRAS, NRAS or PIK3CA mutations and implanted into mice, the therapeutic combination of the MEK inhibitor AZD6244 and the PI3K/… (full text at CIViC) PMID 22392911 · Migliardi et al., 2012 · Open in CIViC	civic

KRAS Mutation7
B-Raf/VEGFR-2 Inhibitor RAF265 + SelumetinibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	accepted	EID989 SiRNA Screening in 37 KRAS Mutant colorectal cancer cell lines identified RAF1 and MEK Inhibition as synergistic, whereas MEK Inhibition alone led to quick resistance via upregulation of RAF-signallin… (full text at CIViC) PMID 25199829 · Lamba et al., 2014 · Open in CIViC	civic
Docetaxel + SelumetinibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	A	Supports Resistance	5	accepted	EID2998 A phase 3 study of selumetinib and docetaxel in KRAS mutant, previously treated NSCLC. 866 were enrolled and 510 randomized. Median progression-free survival was 3.9 months with selumetinib + docetaxe… (full text at CIViC) PMID 28492898 · Jänne et al., 2017 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID999 87 patients with KRAS mutant stage IIB-IV NSCLC after first line therapy were randomly assigned (1:1) to oral selumetunib and docetaxel or docetaxel and Placebo. Median OS was 9·4 months (6·8-13·6) in… (full text at CIViC) PMID 23200175 · Jänne et al., 2013 · Open in CIViC	civic
Erlotinib + SelumetinibCombination	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Does Not Support Sensitivity Response	4	accepted	EID4868 38 KRAS wild-type patients were randomized to erlotinib or combination of selumetinib with erlotinib. 41 KRAS mutant patients were randomized to selumetinib or the combination. The primary end points … (full text at CIViC) PMID 26802155 · Carter et al., 2016 · Open in CIViC	civic
B-Raf/VEGFR-2 Inhibitor RAF265 + SelumetinibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	4	accepted	EID988 SiRNA Screening in 37 KRAS Mutant colorectal cancer cell lines identified RAF1 and MEK Inhibition as synergistic, whereas MEK Inhibition alone led to quick resistance via upregulation of RAF-signallin… (full text at CIViC) PMID 25199829 · Lamba et al., 2014 · Open in CIViC	civic
Cetuximab + SelumetinibCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	B	Does Not Support Sensitivity Response	3	accepted	EID4866 A phase I study to determine the tolerability and pharmacokinetics of Selumetinib and Cetuximab with an expanded cohort in KRAS-mutant CRC. In the KRAS-mutant CRC dose expansion cohort 14 patients we… (full text at CIViC) PMID 26666244 · Deming et al., 2016 · Open in CIViC	civic
Selumetinib + TeprotumumabCombination	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID1004 Preclinial data from KRAS mutant colorectal cancer cell lines show syngergistic effect on cell viability and apoptosis in vitro and in vivo when MEK and IGF-IR are inhibited concomitantly. In other ce… (full text at CIViC) PMID 21985784 · Ebi et al., 2011 · Open in CIViC	civic