Selumetinib
Small molecule targets MAP2K1 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 6 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 ↗ |
| Filed | US (FDA) | — | neurofibromatosis type 1 with plexiform neurofibromas | 2019-11-14 | “the U.S. Food and Drug Administration (FDA) has accepted a New Drug Application (NDA) and granted priority review for the MEK 1/2 inhibitor selumetinib” merck.com ↗ “the US Food and Drug Administration (FDA) has accepted a New Drug Application (NDA) and granted Priority Review for selumetinib” astrazeneca.com ↗ |
Trials 125 · started per year
News releases announcing trial results or a regulatory action · 25
| Date | Issuer | Release |
|---|---|---|
| 2026-04-10 | AstraZeneca | Results Alexion data at 2026 AAN Annual Meeting reflects industry-leading portfolio and commitment to enhancing care across rare diseases astrazeneca.com ↗ |
| 2025-11-20 | AstraZeneca | Regulatory Koselugo approved in the US for adults with neurofibromatosis type 1 astrazeneca.com ↗
Alexion, AstraZeneca Rare Disease’s Koselugo (selumetinib), an oral, selective MEK inhibitor, has been approved in the US for the treatment of adult patients with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN). |
| 2025-10-28 | AstraZeneca | Regulatory Koselugo approved in the EU for plexiform neurofibromas in adults with neurofibromatosis type 1 astrazeneca.com ↗
Alexion, AstraZeneca Rare Disease’s Koselugo (selumetinib), an oral, selective MEK inhibitor, has been approved in the European Union (EU) for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in adult patients with neurofibromatosis type 1 (NF1). |
| 2025-09-22 | AstraZeneca | Regulatory Koselugo recommended for approval in the EU by CHMP for plexiform neurofibromas in adults with neurofibromatosis type 1 astrazeneca.com ↗
Koselugo (selumetinib), an oral, selective MEK inhibitor, has been recommended for approval in the European Union (EU) for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in adult patients with neurofibromatosis type 1 (NF1). |
| 2024-11-12 | Merck Sharp & Dohme LLC | Results KOSELUGO® (selumetinib) Showed Significant and Clinically Meaningful Improvement in Objective Response Rate Versus Placebo in Adults With Neurofibromatosis Type 1 who Have Symptomatic, Inoperable Plexiform Neurofibromas in Global Phase 3 KOMET Trial merck.com ↗
Topline results showed that KOSELUGO, an oral, selective MEK inhibitor, demonstrated a statistically significant and clinically meaningful improvement in objective response rate (ORR), the study’s primary endpoint, versus placebo, in these adult patients. |
| 2024-11-12 | AstraZeneca | Results 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 ↗
These clinically meaningful data show Koselugo has the potential to make a positive impact in patient care by reducing the size of plexiform neurofibromas. |
| 2023-05-08 | AstraZeneca | Regulatory Koselugo approved in China for paediatric patients with neurofibromatosis type 1 and plexiform neurofibromas astrazeneca.com ↗
Koselugo (selumetinib) has been approved in China for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in paediatric patients with neurofibromatosis type 1 (NF1) aged three years and above. |
| 2022-09-27 | AstraZeneca | Regulatory Koselugo approved in Japan for paediatric patients with plexiform neurofibromas in neurofibromatosis type 1 astrazeneca.com ↗ |
| 2021-06-22 | AstraZeneca | Regulatory Koselugo approved in the EU for children with neurofibromatosis type 1 and plexiform neurofibromas astrazeneca.com ↗
AstraZeneca and MSD's Koselugo (selumetinib) has been granted conditional approval in the European Union (EU) for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in paediatric patients with neurofibromatosis type 1 (NF1) aged three years and above. |
| 2021-04-26 | AstraZeneca | Regulatory Selumetinib recommended for approval in the EU by CHMP as the first medicine for paediatric patients with neurofibromatosis type 1 and plexiform neurofibromas astrazeneca.com ↗
AstraZeneca and MSD’s selumetinib has been recommended for conditional marketing authorisation in the European Union (EU) for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in paediatric patients with neurofibromatosis type 1 (NF1) aged three years and above. |
| 2020-06-30 | AstraZeneca | Regulatory Selumetinib granted orphan drug designation in Japan for neurofibromatosis type 1 astrazeneca.com ↗
AstraZeneca today announced that selumetinib has been granted orphan drug designation (ODD) in Japan for the treatment of neurofibromatosis type 1 (NF1), a rare and debilitating genetic disease. |
| 2020-04-13 | Merck Sharp & Dohme LLC | Regulatory KOSELUGO® (selumetinib) Approved by FDA for Pediatric Patients Two Years and Older With Neurofibromatosis Type 1 and Symptomatic, Inoperable Plexiform Neurofibromas merck.com ↗
AstraZeneca and Merck (NYSE: MRK), known as MSD outside the United States and Canada, today announced that the U.S. Food and Drug Administration (FDA) has approved the kinase inhibitor KOSELUGO (selumetinib) for the treatment of pediatric patients two years of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN). |
| 2020-04-13 | AstraZeneca | Regulatory Koselugo (selumetinib) approved in US for paediatric patients with neurofibromatosis type 1 plexiform neurofibromas astrazeneca.com ↗
AstraZeneca and MSD Inc., Kenilworth, N.J., US (MSD: known as Merck & Co., Inc. inside the US and Canada) today announced that the US Food and Drug Administration (FDA) has approved the kinase inhibitor Koselugo (selumetinib) for the treatment of paediatric patients two years of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN). |
| 2019-11-14 | Merck Sharp & Dohme LLC | Regulatory US FDA Accepts Regulatory Submission of New Drug Application for Selumetinib in Neurofibromatosis Type 1 (NF1) and Grants Priority Review merck.com ↗
This is the first acceptance of a regulatory submission for an oral MEK 1/2 monotherapy for patients with NF1, a rare and incurable genetic condition. |
| 2019-11-14 | AstraZeneca | Regulatory US FDA accepts regulatory submission for selumetinib in neurofibromatosis type 1 and grants Priority Review astrazeneca.com ↗
This is the first acceptance of a regulatory submission for an oral monotherapy for the treatment of NF1, a rare and incurable genetic condition. |
| 2019-04-01 | Merck Sharp & Dohme LLC | Regulatory Selumetinib Granted U.S. Breakthrough Therapy Designation in Neurofibromatosis Type 1 merck.com ↗
AstraZeneca and Merck (NYSE: MRK), known as MSD outside the United States and Canada, today announced that the U.S. Food and Drug Administration (FDA) has granted Breakthrough Therapy Designation (BTD) for the investigational MEK 1/2 inhibitor selumetinib. |
| 2019-04-01 | AstraZeneca | Regulatory Selumetinib granted US Breakthrough Therapy Designation in neurofibromatosis type 1 astrazeneca.com ↗ |
| 2018-08-03 | Merck Sharp & Dohme LLC | Regulatory Selumetinib Granted Orphan Designation in Europe for Neurofibromatosis Type 1 merck.com ↗
AstraZeneca and Merck (NYSE:MRK), known as MSD outside the U.S. and Canada, today announced that the European Medicines Agency (EMA) has granted orphan designation to selumetinib, a MEK 1/2 inhibitor, for the treatment of neurofibromatosis type 1 (NF1). |
| 2018-08-03 | AstraZeneca | Regulatory Selumetinib granted orphan designation in Europe for neurofibromatosis type 1 astrazeneca.com ↗ |
| 2018-02-15 | Merck Sharp & Dohme LLC | Regulatory Selumetinib Granted Orphan Drug Designation by the U.S. FDA for Neurofibromatosis Type 1 merck.com ↗
the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for selumetinib, a MEK 1/2 inhibitor, for the treatment of neurofibromatosis type 1 (NF1). |
| 2018-02-15 | AstraZeneca | Regulatory Selumetinib granted Orphan Drug Designation by the US FDA for neurofibromatosis type 1 astrazeneca.com ↗
AstraZeneca and Merck & Co., Inc., Kenilworth, NJ, US (known as MSD outside the US and Canada) today announced that the US Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for selumetinib, a MEK 1/2 inhibitor, for the treatment of neurofibromatosis type 1 (NF1). |
| 2016-08-09 | AstraZeneca | Results AstraZeneca provides update on Phase III trial of Selumetinib in non-small cell lung cancer astrazeneca.com ↗
The results showed that the trial did not meet its primary endpoint of progression-free survival (PFS), and selumetinib did not have a significant effect on overall survival (OS). |
| 2016-05-12 | AstraZeneca | Regulatory Selumetinib granted Orphan Drug Designation in the US for adjuvant treatment of differentiated thyroid cancer astrazeneca.com ↗
AstraZeneca today announced that the US Food and Drug Administration (FDA) has granted Orphan Drug Designation for the investigational MEK 1/2 inhibitor, selumetinib (AZD6244, ARRY-142886) for adjuvant treatment of patients with stage III or IV differentiated thyroid cancer (DTC). |
| 2015-07-22 | AstraZeneca | Results AstraZeneca provides update on selumetinib in uveal melanoma astrazeneca.com ↗
Wednesday, 22 July 2015 AstraZeneca today announced that the Phase III SUMIT study of selumetinib in combination with dacarbazine for the treatment of patients with metastatic uveal melanoma did not meet its primary endpoint of progression free survival. |
| 2015-04-17 | AstraZeneca | Regulatory Selumetinib granted Orphan Drug Designation by US FDA for treatment of uveal melanoma astrazeneca.com ↗
Friday, 17 April 2015 AstraZeneca today announced that the US Food and Drug Administration has granted Orphan Drug Designation for the MEK inhibitor selumetinib, for the treatment of uveal melanoma. |
All press releases naming this drug 26 releases
Evidence & citations 14 cited values
Every value below carries the sentence it was read from. 150 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 ↗ |
| 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 202224“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 |
| 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 |
| 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 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 ↗ |
| Action | Inhibit | “Selumetinib (AZD6244) is an oral, selective, non-ATP-competitive inhibitor of MEK1/2.” PMID 22293660 ↗ Aug 2012 |
| Modality | Small molecule | “Selumetinib is an oral small-molecule inhibitor of MAP-ERK kinase (MEK)-1/2.” PMID 24178622 ↗ Oct 2013 |
| Route | Oral | “Oral liquid or Capsule” NCT00338130 ↗ |
| Target | MAP2K1 | “Selective Mitogen Activated Protein Kinase Kinase (MEK) 1 Inhibitor” NCT04590235 ↗ |