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

Stem definitionDrug idCAS RN
enzyme inhibitors 5823 None

Description:

MoleculeDescription

Molfile

Synonyms:

  • imetelstat
  • rytelo
  • GRN163L
  • JNJ-63935937
  • imetelstat sodium
Imetelstat is an oligonucleotide telomerase inhibitor. Imetelstat binds to the template region of human telomerase RNA (hTR), resulting in inhibition of telomerase activity.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
June 6, 2024 FDA Geron
March 7, 2025 EMA Geron Netherlands B.V.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XX80 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
MeSH PA D004791 Enzyme Inhibitors
FDA EPC N0000194125 Oligonucleotide Telomerase Inhibitor
FDA MoA N0000194126 Oligonucleotide Telomerase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:233423 antifibrotic agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

L01XX Other antineoplastic agents 33 drugs
adagrasibafliberceptaltretamineamsacrineanagrelidearsenic trioxideasparaginasebelzutifancalaspargase pegolcelecoxibdarinaparsindenileukin diftitox show all 33 →

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

DiseaseRelationSNOMED_IDDOID
Low- to intermediate-1 risk myelodysplastic syndrome indication 109995007




🐶 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 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9388415 Sept. 9, 2026 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9388416 Sept. 9, 2026 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9388415 Sept. 9, 2026 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9388416 Sept. 9, 2026 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 12442000 March 15, 2033 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9375485 March 15, 2033 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 12442000 March 15, 2033 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 9375485 March 15, 2033 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 12171778 June 16, 2039 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS 12171778 June 16, 2039 TREATMENT OF PATIENTS WITH MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 188MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS June 6, 2031 TREATMENT OF ADULT PATIENTS WITH LOW - TO INTERMEDIATE-1 RISK MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA REQUIRING 4 OR MORE RED BLOOD CELL UNITS OVER 8 WEEKS WHO HAVE NOT RESPONDED TO OR HAVE LOST RESPONSE TO OR ARE INELIGIBLE FOR ERYTHROPOIESIS-STIMULATING AGENTS (ESA)
EQ 47MG BASE/VIAL RYTELO GERON N217779 June 6, 2024 RX POWDER INTRAVENOUS June 6, 2031 TREATMENT OF ADULT PATIENTS WITH LOW - TO INTERMEDIATE-1 RISK MYELODYSPLASTIC SYNDROMES (MDS) WITH TRANSFUSION-DEPENDENT ANEMIA REQUIRING 4 OR MORE RED BLOOD CELL UNITS OVER 8 WEEKS WHO HAVE NOT RESPONDED TO OR HAVE LOST RESPONSE TO OR ARE INELIGIBLE FOR ERYTHROPOIESIS-STIMULATING AGENTS (ESA)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Telomerase reverse transcriptase Enzyme INHIBITOR IC50 7.25 DRUG LABEL DRUG LABEL

External reference:

IDSource
868169-64-6 SECONDARY_CAS_RN
CHEMBL2107856 ChEMBL_ID
C519562 MESH_SUPPLEMENTAL_RECORD_UI
DB14909 DRUGBANK_ID
DB05036 DRUGBANK_ID
4043215 VANDF
C2746063 UMLSCUI
CHEBI:752899 CHEBI
CHEMBL2108702 ChEMBL_ID
9142 INN_ID
1007380-31-5 SECONDARY_CAS_RN
72941969 PUBCHEM_CID
386208 MMSL
42902 MMSL
d10191 MMSL
019772 NDDF
019773 NDDF
13625 IUPHAR_LIGAND_ID
F60NE4XB53 UNII
2685236 RXNORM
D09629 KEGG_DRUG

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RYTELO HUMAN PRESCRIPTION DRUG LABEL 1 82959-111 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 188 mg INTRAVENOUS NDA 28 sections
RYTELO HUMAN PRESCRIPTION DRUG LABEL 1 82959-112 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 47 mg INTRAVENOUS NDA 28 sections