asciminib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
5495 1492952-76-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • asciminib
  • asciminib hydrochloride
  • scemblix
  • ABL-001
  • ABL-001-NX
  • ABL001-AAA
Asciminib is an ABL/BCR-ABL1 tyrosine kinase inhibitor. Asciminib inhibits the ABL1 kinase activity of the BCR­ABL1 fusion protein, by binding to the ABL myristoyl pocket. In studies conducted in vitro or in animal models of CML, asciminib showed activity against wild-type BCR-ABL1 and several mutant forms of the kinase, including the T315I mutation.
  • Molecular weight: 449.84
  • Formula: C20H18ClF2N5O3
  • CLOGP: 3.64
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 103.37
  • ALOGS: -3.91
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
80 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class EIF2AK3,PDK1,PDK2,PDK4 4
kinase-selectivity-class EIF2AK3 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Oct. 29, 2021 FDA NOVARTIS
March 24, 2020 EMA Novartis Europharm Limited
March 28, 2022 PMDA Novartis Pharma K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cytopenia 97.66 40.59 28 1640 17421 90609358
Cytogenetic analysis abnormal 92.22 40.59 16 1652 994 90625785
Thrombocytopenia 85.40 40.59 51 1617 208674 90418105
Pleural effusion 69.38 40.59 36 1632 111955 90514824
Philadelphia chromosome positive 67.22 40.59 11 1657 479 90626300
Graft versus host disease in eye 57.32 40.59 8 1660 116 90626663
Blast crisis in myelogenous leukaemia 57.16 40.59 10 1658 651 90626128
Lipase increased 54.04 40.59 16 1652 11095 90615684
Drug intolerance 48.93 40.59 50 1618 447541 90179238
Pericardial effusion 48.48 40.59 20 1648 36813 90589966
Platelet count abnormal 43.31 40.59 11 1657 4324 90622455
Loss of therapeutic response 41.74 40.59 9 1659 1743 90625036
Drug resistance 41.65 40.59 17 1651 30432 90596347
Malignant neoplasm progression 40.69 40.59 25 1643 106845 90519934

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Philadelphia chromosome positive 111.27 33.01 20 1869 621 42618825
Drug intolerance 65.56 33.01 42 1847 80382 42539064
Thrombocytopenia 62.93 33.01 58 1831 190221 42429225
Cytopenia 62.76 33.01 25 1864 17472 42601974
Cytogenetic analysis abnormal 52.53 33.01 11 1878 764 42618682
Hepatotoxicity 50.91 33.01 24 1865 25143 42594303
Pleural effusion 49.35 33.01 38 1851 97128 42522318
Lipase increased 44.60 33.01 17 1872 10549 42608897
Blast cell crisis 43.18 33.01 7 1882 115 42619331
Blast crisis in myelogenous leukaemia 42.53 33.01 9 1880 657 42618789
Acute lymphocytic leukaemia recurrent 39.75 33.01 12 1877 3679 42615767
Pericardial effusion 33.38 33.01 19 1870 29256 42590190

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Thrombocytopenia 105.75 34.04 77 2479 348808 110237935
Philadelphia chromosome positive 103.82 34.04 18 2538 882 110585861
Pleural effusion 97.59 34.04 57 2499 177652 110409091
Cytogenetic analysis abnormal 84.91 34.04 16 2540 1253 110585490
Lipase increased 77.03 34.04 25 2531 18647 110568096
Blast crisis in myelogenous leukaemia 69.27 34.04 13 2543 995 110585748
Loss of therapeutic response 68.43 34.04 15 2541 2495 110584248
Malignant neoplasm progression 65.48 34.04 44 2512 174523 110412220
Pericardial effusion 65.14 34.04 30 2526 57187 110529556
Drug intolerance 63.03 34.04 61 2495 406451 110180292
Cytopenia 61.77 34.04 24 2532 30092 110556651
Graft versus host disease in eye 45.01 34.04 8 2548 452 110586291
Acute lymphocytic leukaemia recurrent 42.12 34.04 12 2544 5775 110580968
Chronic myeloid leukaemia recurrent 39.48 34.04 7 2549 390 110586353
Blast cell crisis 37.89 34.04 6 2550 167 110586576
Platelet count decreased 36.40 34.04 35 2521 230408 110356335
Pulmonary hypertension 36.38 34.04 20 2536 55200 110531543
Chronic myeloid leukaemia transformation 34.15 34.04 6 2550 317 110586426

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EA06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
BCR-ABL tyrosine kinase inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L01EA BCR-ABL tyrosine kinase inhibitors 5 drugs
bosutinibdasatinibimatinibnilotinibponatinib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) indication 92818009 DOID:8552




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE SCEMBLIX NOVARTIS N215358 April 18, 2024 RX TABLET ORAL 8829195 Oct. 29, 2035 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 8829195 Oct. 29, 2035 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 8829195 Oct. 29, 2035 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 100MG BASE SCEMBLIX NOVARTIS N215358 April 18, 2024 RX TABLET ORAL 12252479 May 17, 2040 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 12252479 May 17, 2040 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 12252479 May 17, 2040 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE SCEMBLIX NOVARTIS N215358 April 18, 2024 RX TABLET ORAL Oct. 29, 2026 NEW CHEMICAL ENTITY
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2026 NEW CHEMICAL ENTITY
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2026 NEW CHEMICAL ENTITY
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP)
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2027 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2027 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2027 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP)
EQ 100MG BASE SCEMBLIX NOVARTIS N215358 April 18, 2024 RX TABLET ORAL Oct. 2, 2028 MODIFICATIONS TO LABELING TO INCLUDE UPDATED RECOMMENDATIONS FOR CYP3A4 INDUCERS AND SUBSTRATES OF BCRP AND UPDATED DATA FOR STRONG CYP3A4 INDUCERS AND OATP1B SUBSTRATES
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 2, 2028 MODIFICATIONS TO LABELING TO INCLUDE UPDATED RECOMMENDATIONS FOR CYP3A4 INDUCERS AND SUBSTRATES OF BCRP AND UPDATED DATA FOR STRONG CYP3A4 INDUCERS AND OATP1B SUBSTRATES
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 2, 2028 MODIFICATIONS TO LABELING TO INCLUDE UPDATED RECOMMENDATIONS FOR CYP3A4 INDUCERS AND SUBSTRATES OF BCRP AND UPDATED DATA FOR STRONG CYP3A4 INDUCERS AND OATP1B SUBSTRATES
EQ 100MG BASE SCEMBLIX NOVARTIS N215358 April 18, 2024 RX TABLET ORAL Oct. 29, 2028 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2028 TREATMENT OF ADULT PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), PREVIOUSLY TREATED WITH TWO OR MORE TYROSINE KINASE INHIBITORS (TKIS)
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2028 TREATMENT OF ADULT PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP) WITH THE T315I MUTATION
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2028 TREATMENT OF ADULT PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), PREVIOUSLY TREATED WITH TWO OR MORE TYROSINE KINASE INHIBITORS (TKIS)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2028 TREATMENT OF ADULT PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP) WITH THE T315I MUTATION
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), EXCLUDING PATIENTS WITH THE T315I MUTATION
EQ 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2031 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), EXCLUDING PATIENTS PREVIOUSLY TREATED WITH TWO OR MORE TYROSINE KINASE INHIBITORS (TKIS), AND EXCLUDING PATIENTS WITH THE T315I MUTATION
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2031 TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), EXCLUDING PATIENTS WITH THE T315I MUTATION
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL Oct. 29, 2031 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED PHILADELPHIA CHROMOSOME-POSITIVE CHRONIC MYELOID LEUKEMIA (PH+ CML) IN CHRONIC PHASE (CP), EXCLUDING PATIENTS PREVIOUSLY TREATED WITH TWO OR MORE TYROSINE KINASE INHIBITORS (TKIS), AND EXCLUDING PATIENTS WITH THE T315I MUTATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase ABL1 Kinase INHIBITOR IC50 8.59 DRUG LABEL DRUG LABEL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.58 CHEMBL

External reference:

IDSource
CHEBI:756638 CHEBI
AY7 PDB_CHEM_ID
CHEMBL4208229 ChEMBL_ID
C000621806 MESH_SUPPLEMENTAL_RECORD_UI
8962 IUPHAR_LIGAND_ID
DB12597 DRUGBANK_ID
4040935 VANDF
C4508722 UMLSCUI
D11403 KEGG_DRUG
CHEMBL4297220 ChEMBL_ID
10267 INN_ID
2119669-71-3 SECONDARY_CAS_RN
72165228 PUBCHEM_CID
353164 MMSL
40068 MMSL
d09827 MMSL
018882 NDDF
018883 NDDF
L1F3R18W77 UNII
2584303 RXNORM
L1F3R18W77 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1091 TABLET, FILM COATED 20 mg ORAL NDA 30 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1091 TABLET, FILM COATED 20 mg ORAL NDA 30 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1098 TABLET, FILM COATED 40 mg ORAL NDA 30 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1098 TABLET, FILM COATED 40 mg ORAL NDA 30 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1196 TABLET, FILM COATED 100 mg ORAL NDA 30 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1196 TABLET, FILM COATED 100 mg ORAL NDA 30 sections