Momelotinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Momelotinib
- Molecular weight
- 414.47
- Structure (SMILES)
- N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1
- cyt 0387
- cyt 11387
- cyt 387
- CYT-0387
- CYT-11387
- Cyt-387
- CYT-387
- cyt387
- CYT387
- gs 0387
- GS-0387
- momelotinib
- Momelotinib
- Momelotinib (MMB)
- momelotinib [INN]
- Momelotinib [MI]
- MOMELOTINIB [USAN]
- Momelotinib [WHO-DD]
- momelotinib inn
- momelotinib mi
- momelotinib usan
- momelotinib who dd
- ATC classification codes
- L01EJ04
Sources for recorded values
- CAS registry numbers
- 1056634-68-4
- ChEMBL ID
- CHEMBL1078178
- InChIKey
- ZVHNDZWQTBEVRY-UHFFFAOYSA-N
- PubChem compound IDs
- 25062766
- RxNorm IDs (RxCUI)
- 2665204
- FDA ingredient codes (UNII)
- 6O01GMS00P
- Applicant
- GLAXOSMITHKLINE
- Approval date
- 15 Sept 2023
- Application number
- NDA216873
- Status
- Authorised
- Status date
- 25 Jan 2024
- Authorisation date
- 25 Jan 2024
- Approved indications
- Omjjara is indicated for the treatment of disease-related splenomegaly or symptoms in adult patients with moderate to severe anaemia who have primary myelofibrosis, post polycythaemia vera myelofibrosis or post essential thrombocythaemia myelofibrosis and who are Janus Kinase (JAK) inhibitor naïve or have been treated with ruxolitinib.
- Product number
- EMEA/H/C/005768
- Authorisation holder
- GlaxoSmithKline Trading Services Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Myeloproliferative Disorders
- Splenomegaly
European medicines record
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- Yes
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- momelotinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 2
- Gene symbol
- JAK2
- Protein identifier
- O60674
- Median affinity
- 8.85
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 1
- Gene symbol
- JAK1
- Protein identifier
- P23458
- Median affinity
- 7.57
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tyrosine kinase 2
- Gene symbol
- TYK2
- Protein identifier
- P29597
- Median affinity
- 7.7
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 3
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Median affinity
- 6.81
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- activin A receptor type 1
- Gene symbol
- ACVR1
- Protein identifier
- Q04771
- Median affinity
- 8.08
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase JAK1 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK1
- Protein identifier
- P23458
- Mechanism
- Tyrosine-protein kinase JAK2 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK2
- Protein identifier
- O60674
- Mechanism
- Activin receptor type-1 inhibitor
- Action type
- Inhibitor
- Target
- Activin receptor type-1
- Mechanism
- Tyrosine-protein kinase JAK1 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK1
- Mechanism
- Tyrosine-protein kinase JAK2 inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase JAK2
- Condition
- Thrombocythemia, Essential
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000479
- Subject identifier
- D013920
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Polycythemia Vera
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002429
- Subject identifier
- D011087
- Condition
- Primary Myelofibrosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002430
- Subject identifier
- D055728
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Leukemia, Myeloid
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004643
- Subject identifier
- D007951
- Condition
- Carcinoma, Pancreatic Ductal
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0005184
- Subject identifier
- D021441
- Condition
- Primary Myelofibrosis
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0044903
- Subject identifier
- D055728
- Condition identifier
- EFO_0000198
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0002429
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002430
- Highest recorded phase
- 3
- Condition identifier
- EFO_0004251
- Condition identifier
- HP_0001744
- Condition identifier
- HP_0001894
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005029
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005184
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0006311
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0009692
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0009891
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018874
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0018881
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0019111
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0019451
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0020311
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0026777
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0044903
- Condition identifier
- MONDO_0044903
- Highest recorded phase
- 4
- Event
- respiratory tract infection
- Reports
- 3
- Reporting signal score
- 13.1696
- Event
- splenomegaly
- Reports
- 3
- Reporting signal score
- 15.2803
- NCT01236638
- NCT01423058
- NCT01969838
- NCT02101268
- NCT02124746
- NCT01998828
- NCT02101021
- NCT02244489
- NCT02206763
- NCT02258607
- NCT06235801
- Dose
- 200 mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- With or without food
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 2
- Polar surface area
- 103.17
- Calculated partition coefficient (ALogP)
- 2.98
- Calculated partition coefficient (XLogP)
- 2.6
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 31
- Molecular formula
- C23H22N6O2
- Monoisotopic mass
- 414.18042397
- Natural product
- Yes
- Recorded assays
- 2,488
- Active assays
- 391
- Confirmatory
- Other
- Screening
- Janus Kinase Inhibitors
- Antineoplastic Agents
Solubility
- Median
- 0.2
- Mean
- 65.65
- Minimum
- 0.2
- Maximum
- 262
- Unit
- ug/mL
- Assays
- 4
- Standard deviation
- 130.9
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Oral bioavailability
- Median
- 24
- Mean
- 24
- Minimum
- 24
- Maximum
- 24
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Plasma protein binding
- Median
- 91
- Mean
- 91
- Minimum
- 91
- Maximum
- 91
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- PPB
Related records
Trials (26)
- A Phase I/II Study of Gilteritinib and Momelotinib for Patients With Relapsed or Refractory FLT3-Mutated Acute Myeloid Leukemia
- A Study Evaluating the Efficacy and Safety of Momelotinib in Participants With Vacuoles, E1-enzyme, X-linked, Autoinflammatory, Somatic (VEXAS) Syndrome
- A Study of JNJ-88549968 for the Treatment of Calreticulin (CALR)-Mutated Myeloproliferative Neoplasms
- A Study of Momelotinib in Participants With Low-risk Myelodysplastic Syndrome
- A Study of Momelotinib Versus Danazol in Symptomatic and Anemic Myelofibrosis Participants (MOMENTUM)
- A Study of Oral Nuvisertib (TP-3654) in Patients With Myelofibrosis
- A Study of Selinexor Monotherapy in Subjects With JAK Inhibitor-naïve Myelofibrosis and Moderate Thrombocytopenia
- Comparing Momelotinib and Ruxolitinib in People With Untreated Myelofibrosis and Low Blood Cell Counts
- Efficacy and Safety of Momelotinib Combined With Trametinib in Adults With Metastatic KRAS-mutated Non-Small Cell Lung Cancer (NSCLC) Who Have Failed Platinum-Based Chemotherapy Preceded by a Dose-finding Lead-in Phase
- Efficacy of Momelotinib Versus Best Available Therapy in Anemic or Thrombocytopenic Subjects With Primary Myelofibrosis (MF), Post-polycythemia Vera MF, or Post-essential Thrombocythemia MF
- Erlotinib and Momelotinib for the Treatment of Epidermal Growth Factor Receptor (EGFR) Mutated EGFR Tyrosine Kinase Inhibitor (TKI) Naive Metastatic Non-Small Cell Lung Cancer (NSCLC)
- Extended Access of Momelotinib in Adults With Myelofibrosis
- Extension Study Evaluating the Long Term Safety and Efficacy Study of CYT387 in Primary Myelofibrosis (PMF) or Post-polycythemia Vera (PV) or Post-essential Thrombocythemia (ET)
- Gemcitabine and Nab-paclitaxel Combined With Momelotinib in Participants With Previously Untreated Metastatic Pancreatic Ductal Adenocarcinoma
- Long-term Safety and Efficacy of Momelotinib in Subjects With Primary Myelofibrosis, Post-polycythemia Vera Myelofibrosis, Post-essential Thrombocythemia Myelofibrosis, Polycythemia Vera or Essential Thrombocythemia
- Managed Access Program for Momelotinib in Myelofibrosis
- Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma
- Momelotinib During and After HCT in Myelofibrosis
- Momelotinib in Combination With Hypomethylating Agent for Chronic Phase Myelodysplastic Syndromes/Myeloproliferative Overlap Neoplasms and Chronic Neutrophilic Leukemia
- Momelotinib in Transfusion-Dependent Adults With Primary Myelofibrosis (PMF) or Post-polycythemia Vera or Post-essential Thrombocythemia Myelofibrosis (Post-PV/ET MF)
In development for (10)
- Acquired polycythemia vera Phase 2
- Essential thrombocythemia Phase 2
- Familial thrombocytosis Phase 2
- Myelodysplastic syndrome Phase 2
- Myelofibrosis Phase 3
- Myeloid leukemia Phase 1
- Neoplasm Phase 3
- Non-small cell lung carcinoma Phase 1
- Pancreatic ductal adenocarcinoma Phase 3
- Primary myelofibrosis Phase 3