asciminib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 24, 2020 EMA Novartis Europharm Limited
Oct. 29, 2021 FDA NOVARTIS
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
Cytogenetic analysis abnormal 104.20 42.34 15 359 905 63487743

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
Cytopenia 59.86 41.04 17 505 12706 34943703

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
Cytogenetic analysis abnormal 61.66 36.75 10 513 1180 79742685
Renal failure 38.83 36.75 21 502 200947 79542918

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

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 20MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 8829195 May 13, 2033 TREATMENT OF PHILADELPHIA CHROMOSOME POSITIVE CHRONIC MYELOID LEUKEMIA (PH+CML)
EQ 40MG BASE SCEMBLIX NOVARTIS N215358 Oct. 29, 2021 RX TABLET ORAL 8829195 May 13, 2033 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 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, 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

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1091 TABLET, FILM COATED 20 mg ORAL NDA 29 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1091 TABLET, FILM COATED 20 mg ORAL NDA 29 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1091 TABLET, FILM COATED 20 mg ORAL NDA 29 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1098 TABLET, FILM COATED 40 mg ORAL NDA 29 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1098 TABLET, FILM COATED 40 mg ORAL NDA 29 sections
SCEMBLIX HUMAN PRESCRIPTION DRUG LABEL 1 0078-1098 TABLET, FILM COATED 40 mg ORAL NDA 29 sections