Selumetinib
Small molecule targets MAP2K1, MAP2K2 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 5 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Label expansions (3) | US (FDA) | KOSELUGO | — | 2024-01-24 – 2025-11-19 | fda.gov ↗ |
| Approved · conditional | EU (EMA) | Koselugo | — | 2021-06-17 | europa.eu ↗ |
| Approved | US (FDA) | KOSELUGO | — | 2020-04-10 | fda.gov ↗ |
Trials 127 · started per year
Also used as a comparator or background therapy in 7 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 27 trials | ||||||
| Phase 2 | NCT05825365 Comparator | Aug 2023 → Jun 2026 | neurofibromatosis type 1, plexiform neurofibroma | AstraZeneca | Withdrawn | No outcome recorded |
| Phase 2 | NCT02337530 Comparator | May 2015 → Oct 2017 | non-small cell lung carcinoma | Canadian Cancer Trials Group | Completed | No outcome recorded |
| Phase 2 | NCT01306045 Comparator | Feb 2011 → Feb 2014 | non-small cell lung carcinoma, small cell lung carcinoma, thymic carcinoma | National Cancer Institute (NCI) | Completed | No outcome recorded |
| Phase 2 | NCT01229150 Comparator | Oct 2010 → Sep 2013 | non-small cell lung carcinoma | National Cancer Institute (NCI) | Completed | No outcome recorded |
| Phase 2 | NCT01160718 Comparator | Aug 2010 → Dec 2012 | female breast carcinoma | Swiss Cancer Institute | Completed | No outcome recorded |
| Phase 2 | NCT00936221 Comparator | Jul 2009 → Nov 2011 | melanoma | AstraZeneca | Completed | No outcome recorded |
| Phase 2 | NCT00890825 Comparator | Apr 2009 → May 2011 | non-small cell lung carcinoma | AstraZeneca | Completed | No outcome recorded |
Press releases naming this drug 4 releases
| Date | Issuer | Release |
|---|---|---|
| 2025-11-20 | AstraZeneca | Koselugo approved in the US for adults with neurofibromatosis type 1 astrazeneca.com ↗ |
| 2025-10-28 | AstraZeneca | Koselugo approved in the EU for plexiform neurofibromas in adults with neurofibromatosis type 1 astrazeneca.com ↗ |
| 2025-09-22 | AstraZeneca | Koselugo recommended for approval in the EU by CHMP for plexiform neurofibromas in adults with neurofibromatosis type 1 astrazeneca.com ↗ |
| 2024-11-12 | AstraZeneca | Koselugo showed statistically significant and clinically meaningful objective response rate vs. placebo in adults with neurofibromatosis type 1 in global KOMET Phase III trial astrazeneca.com ↗ |
Evidence & citations 22 cited values
Every value below carries the sentence it was read from. 153 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Selumetinib | “Selumetinib (ARRY-142886) is an oral, potent, and highly selective allosteric mitogen-activated protein kinase kinase 1/2 inhibitor approved for the treatment of pediatric...” PMID 35410754 ↗ Apr 2022112“Selumetinib (AZD6244 or ARRY-142886), an oral selective inhibitor of MAPK kinase (MEK) 1 and 2, in children who had neurofibromatosis type 1 and inoperable plexiform...” PMID 28029918 ↗ Dec 2016 “We conducted a study to determine whether the MAPK kinase (MEK) 1 and MEK2 inhibitor selumetinib (AZD6244, ARRY-142886) could reverse refractoriness to radioiodine in patients...” PMID 23406027 ↗ Feb 2013 “Selumetinib (AZD6244, ARRY-142886), an oral, potent, and highly selective mitogen-activated protein kinase 1/2 inhibitor with a short half-life, has shown activity across...” PMID 28985960 ↗ Oct 2017 “A phase I study of selumetinib (AZD6244/ARRY-142866), a MEK1/2 inhibitor, in combination with cetuximab in refractory solid tumors and KRAS mutant colorectal cancer.” PMID 26666244 ↗ Dec 2015 “Selumetinib (AZD6244; ARRY-142886) is an oral selective MEK kinase inhibitor of the Ras/Raf/MEK/ERK pathway.” PMID 26802155 ↗ Jan 2016 “Selumetinib (AZD6244, ARRY-142886) is an oral, potent and highly selective, allosteric inhibitor of MEK1/2” PMID 28424891 ↗ Apr 2017 “Selumetinib (AZD6244) is an oral, selective, non-ATP-competitive inhibitor of MEK1/2.” PMID 22293660 ↗ Aug 2012 “A phase Ib study of selumetinib (AZD6244, ARRY-142886) in combination with” PMID 27681866 ↗ Sep 2016 “MEK Inhibitors (Trametinib 2 mg/d, Selumetinib 75 mg 2/d)” NCT05063058 ↗ “Selumetinib” NCT01931761 ↗ “Selumetinib” NCT06727357 ↗ |
| Known as | ARRAY142886 | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Known as | ARRY-142866 | “A phase I study of selumetinib (AZD6244/ARRY-142866), a MEK1/2 inhibitor, in combination with cetuximab in refractory solid tumors and KRAS mutant colorectal cancer.” PMID 26666244 ↗ Dec 2015 |
| Known as | ARRY-142886 | “Selumetinib (ARRY-142886) is an oral, potent, and highly selective allosteric mitogen-activated protein kinase kinase 1/2 inhibitor approved for the treatment of pediatric...” PMID 35410754 ↗ Apr 202225“A Phase I, Open Label, Multicentre Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of Selumetinib (AZD6244; ARRY-142886) in Combination With...” NCT01809210 ↗ “Selumetinib (AZD6244 or ARRY-142886), an oral selective inhibitor of MAPK kinase (MEK) 1 and 2, in children who had neurofibromatosis type 1 and inoperable plexiform...” PMID 28029918 ↗ Dec 2016 “A Phase I, Open-Label, Multi-Center Study to Assess the Safety and Tolerability of Selumetinib (AZD6244, ARRY-142886) in Combination With Cisplatin/Gemcitabine in Japanese...” NCT01949870 ↗ “A Phase I, Single-centre, Open-label, Dose-escalation Study to Assess the Safety, Tolerability and Pharmacokinetics of Selumetinib (AZD6244; ARRY-142886) (Hyd-Sulfate) Given...” NCT01960374 ↗ “We conducted a biomarker-driven trial of selumetinib (KOSELUGO™; ARRY-142886), an orally active, allosteric mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, in...” PMID 33405090 ↗ Jan 2021 “We conducted a study to determine whether the MAPK kinase (MEK) 1 and MEK2 inhibitor selumetinib (AZD6244, ARRY-142886) could reverse refractoriness to radioiodine in patients...” PMID 23406027 ↗ Feb 2013 “Selumetinib (AZD6244, ARRY-142886) is an oral, potent, and selective MEK1/2 inhibitor with a short half-life, which demonstrated single-agent activity in patients with...” PMID 29528792 ↗ Mar 2018 “Selumetinib (AZD6244, ARRY-142886), an oral, potent, and highly selective mitogen-activated protein kinase 1/2 inhibitor with a short half-life, has shown activity across...” PMID 28985960 ↗ Oct 2017 “The capsule and granule formulations of selumetinib (ARRY-142886, AZD6244) are approved for pediatric patients with symptomatic, inoperable NF1-PN (age ≥1 to 3 years, region dependent).” PMID 41592259 ↗ Jan 2026 “Selumetinib (AZD6244, ARRY142886), a MEK1/2 inhibitor combined with chemotherapy in patients with NSCLC was evaluated in two schedules to evaluate efficacy and toxicity.” PMID 31200828 ↗ May 2019 “To Assess the Effects of Single Oral Dose of Selumetinib \[AZD6244; ARRY-142886\] \[Hyd-Sulfate\]), on QTc Interval in Healthy Male Volunteers” NCT02056392 ↗ “Selumetinib (AZD6244, ARRY-142886) potently and selectively inhibits MEK1/2, an intracellular kinase and has shown activity in ABC.” PMID 26912134 ↗ Feb 2016 “Selumetinib (AZD6244, ARRY-142886) is an orally available, potent, selective, non-ATP competitive inhibitor of MEK1/MEK2 kinases.” NCT02583542 ↗ “Selumetinib (AZD6244, ARRY-142886) is a potent inhibitor of MEK1/2, thereby inhibiting phosphorylation of ERK2.” PMID 30317534 ↗ Oct 2018 “The KOMET study aimed to evaluate selumetinib (ARRY-142886, AZD6244) efficacy and safety in this population.” PMID 40473450 ↗ Jun 2025 “Selumetinib (AZD6244; ARRY-142886) is an oral selective MEK kinase inhibitor of the Ras/Raf/MEK/ERK pathway.” PMID 26802155 ↗ Jan 2016 “Selumetinib (AZD6244, ARRY-142886)+docetaxel increases median overall survival (OS)” PMID 26125448 ↗ Jun 2015 “Selumetinib (AZD6244, ARRY-142886), an oral mitogen activated kinase 1/2 inhibitor” PMID 27751676 ↗ Oct 2016 “Selumetinib (AZD6244; ARRY-142886) (Hyd-Sulfate) in Combination With Docetaxel” NCT01750281 ↗ “Selumetinib (AZD6244, ARRY 142886) (Hyd Sulfate) Following a Single Oral Dose” NCT02063204 ↗ “A phase Ib study of selumetinib (AZD6244, ARRY-142886) in combination with” PMID 27681866 ↗ Sep 2016 “novel therapeutics (AZD6094 or selumetinib (AZD6244, ARRY142886))” NCT02143466 ↗ “allosteric MEK1/2 inhibitor selumetinib (AZD6244; ARRY-142886)” PMID 25516890 ↗ Dec 2014 “Selumetinib (AZD6244, ARRY-142886) (Hyd-Sulfate)” NCT02063230 ↗ |
| Known as | ARRY-886 | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Known as | AZ6244 | ClinicalTrials.gov intervention name — accepted as the source's own label NCT01313039 ↗ |
| Known as | Azd-6244 hydrogen sulphate | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Known as | AZD6244 | “A Phase I, Open Label, Multicentre Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of Selumetinib (AZD6244; ARRY-142886) in Combination With...” NCT01809210 ↗40“Selumetinib (AZD6244 or ARRY-142886), an oral selective inhibitor of MAPK kinase (MEK) 1 and 2, in children who had neurofibromatosis type 1 and inoperable plexiform...” PMID 28029918 ↗ Dec 2016 “A Phase I, Open-Label, Multi-Center Study to Assess the Safety and Tolerability of Selumetinib (AZD6244, ARRY-142886) in Combination With Cisplatin/Gemcitabine in Japanese...” NCT01949870 ↗ “A Phase I, Single-centre, Open-label, Dose-escalation Study to Assess the Safety, Tolerability and Pharmacokinetics of Selumetinib (AZD6244; ARRY-142886) (Hyd-Sulfate) Given...” NCT01960374 ↗ “Selumetinib (AZD6244, ARRY-142886) is an oral, potent, and selective MEK1/2 inhibitor with a short half-life, which demonstrated single-agent activity in patients with...” PMID 29528792 ↗ Mar 2018 “The capsule and granule formulations of selumetinib (ARRY-142886, AZD6244) are approved for pediatric patients with symptomatic, inoperable NF1-PN (age ≥1 to 3 years, region dependent).” PMID 41592259 ↗ Jan 2026 “Selumetinib (AZD6244, ARRY142886), a MEK1/2 inhibitor combined with chemotherapy in patients with NSCLC was evaluated in two schedules to evaluate efficacy and toxicity.” PMID 31200828 ↗ May 2019 “Module G will investigate the safety and tolerability of MEDI4736 given intravenously in combination with selumetinib (AZD6244) given orally to patients with MIBC.” NCT02546661 ↗ “MEK 1/2 Inhibitor Selumetinib (AZD6244 Hydrogen Sulfate) in Adults With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas” NCT02407405 ↗ “A Phase I Trial of Vandetanib (AZD6474) and Selumetinib (AZD6244) for Solid Tumours Including Non Small Cell Lung Cancer (VanSel-1)” NCT01586624 ↗ “Selumetinib (AZD6244, ARRY-142886) is a potent inhibitor of MEK1/2, thereby inhibiting phosphorylation of ERK2.” PMID 30317534 ↗ Oct 2018 “Selumetinib (AZD6244, ARRY-142886), an oral mitogen activated kinase 1/2 inhibitor” PMID 27751676 ↗ Oct 2016 “Selumetinib (AZD6244; ARRY-142886) (Hyd-Sulfate) in Combination With Docetaxel” NCT01750281 ↗ “Selumetinib (AZD6244, ARRY 142886) (Hyd Sulfate) Following a Single Oral Dose” NCT02063204 ↗ “novel therapeutics (AZD6094 or selumetinib (AZD6244, ARRY142886))” NCT02143466 ↗ “Selumetinib (AZD6244, ARRY-142886) (Hyd-Sulfate)” NCT02063230 ↗ “Selumetinib (AZD6244)” NCT03649165 ↗ |
| Known as | AZD6244 (SELUMETINIB) | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Known as | AZD6244 hyd sulfate | “Selumetinib (AZD6244 hyd sulfate), a novel orally bioavailable mitogen activated protein kinase inhibitor, is a specific inhibitor of MEK 1, which may mediate anti-tumor...” NCT01362803 ↗2“Ascending Doses of Selumetinib (AZD6244 Hyd-sulfate) in Combination With MEDI4736” NCT02586987 ↗ “Selumetinib (AZD6244 hyd sulfate) 50mg/dose” NCT03109301 ↗ |
| Known as | AZD6244 Hyd-Sulphate | “Phase I/II Study of Oral MEK Inhibitor Selumetinib (AZD6244 Hyd-Sulphate) in Combination With Highly Active Anti-Retroviral Therapy (HAART) in AIDS-associated Kaposi's Sarcoma (KS).” NCT01752569 ↗ |
| Known as | AZD6244 Hydrogen Sulfate | “MEK 1/2 Inhibitor Selumetinib (AZD6244 Hydrogen Sulfate) in Adults With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas” NCT02407405 ↗3“Selumetinib (AZD6244 Hydrogen Sulfate) in People With Neurofibromatosis Type 1 (NF1) Mutated Gastrointestinal Stromal Tumors (GIST)” NCT03109301 ↗ “receiving the combination of AZD6244 hydrogen sulfate (selumetinib) and MK-2206 (Akt inhibitor MK-2206).” NCT01859182 ↗ “selumetinib (AZD6244 hydrogen sulfate)” NCT07619521 ↗ |
| Known as | KOSELUGO | “We conducted a biomarker-driven trial of selumetinib (KOSELUGO™; ARRY-142886), an orally active, allosteric mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, in...” PMID 33405090 ↗ Jan 2021 |
| Known as | Selumetinib (AZD6244) | “Selumetinib (AZD6244)” NCT01605916 ↗ |
| Known as | Selumetinib hydrogen sulfate | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Known as | selumetinib sulfate | “I. Determine if selumetinib sulfate (selumetinib) can result in shrinkage of cutaneous neurofibromas.” NCT02839720 ↗6“selumetinib sulfate (selumetinib) administered as 75 mg orally twice daily on a continuous schedule” NCT03040986 ↗ “Cediranib Maleate and Selumetinib Sulfate in Treating Patients With Solid Malignancies” NCT01364051 ↗ “Drug: Selumetinib Sulfate” NCT05554328 ↗ “Drug: Selumetinib Sulfate” NCT03213691 ↗ “Drug: Selumetinib Sulfate” NCT00551070 ↗ |
| Known as | Selumetinib sulphate | ChEMBL registry synonym — accepted as the source's own label CHEMBL1614701 ↗ |
| Action | Inhibit | “Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL1614701 ↗1“ARRY-142886, MEK inhibitor; oral” NCT00085787 ↗ |
| Modality | Small molecule | “Selumetinib is an oral small-molecule inhibitor of MAP-ERK kinase (MEK)-1/2.” PMID 24178622 ↗ Oct 2013 |
| Route | Oral | “ARRY-142886, MEK inhibitor; oral” NCT00085787 ↗ |
| Target | MAP2K1 | “Selective Mitogen Activated Protein Kinase Kinase (MEK) 1 Inhibitor” NCT04590235 ↗ |
| Target | MAP2K2 | “Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL1614701 ↗ |