General Information of Drug (ID: DM7UP8X)

Drug Name
Pegfilgrastim
Synonyms Neulasta; Neulasta (TN); Pegfilgrastim (INN)
Indication
Disease Entry ICD 11 Status REF
Central nervous system neoplasm N.A. Approved [1]
Hemoglobinopathy N.A. Approved [2]
Lymphoma 2A80-2A86 Approved [3]
Malignant solid tumour 2C10-2F32 Approved [4]
MALT lymphoma N.A. Approved [2]
Nodal marginal zone lymphoma 2A85.0 Approved [2]
Non-small-cell lung cancer 2C25.Y Approved [5]
Plasma cell myeloma 2A83.1 Approved [6]
Splenic marginal zone lymphoma N.A. Approved [2]
Thalassemia 3A50 Approved [7]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Immunomodulatory Agents
Drug Type
Small molecular drug
Sequence
MTPLGPASSLPQSFLLKCLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWA
PLSSCPSQALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQ
QMEELGMAPALQPTQGAMPAFASAFQRRAGGVLVASHLQSFLEVSYRVLRHLAQP
Structure
3D MOL is unavailable 2D MOL
#Ro5 Violations (Lipinski): 5 Molecular Weight (mw) 730.7
Logarithm of the Partition Coefficient (xlogp) -8.6
Rotatable Bond Count (rotbonds) 19
Hydrogen Bond Donor Count (hbonddonor) 12
Hydrogen Bond Acceptor Count (hbondacc) 20
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 360 mcgh/L [8]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 21 mcg/L [8]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 4-5 h [8]
Bioavailability
The bioavailability of drug is 80% [8]
Clearance
The clearance of drug is 14 mL/h/kg [9]
Half-life
The concentration or amount of drug in body reduced by one-half in 15 - 80 hours [10]
Metabolism
The drug is metabolized via the neutrophil and undergoes nonspecific degradation [11]
Vd
The volume of distribution (Vd) of drug is 170 L []
Chemical Identifiers
Formula
C27H46N4O19
IUPAC Name
(2R,4S,5R,6R)-2-[[(2R,3R,4R,5R,6S)-5-acetamido-6-[(1S,2R)-1-amino-1-carboxypropan-2-yl]oxy-3,4-dihydroxyoxan-2-yl]methoxy]-4-hydroxy-5-[[2-(2-methoxyethoxycarbonylamino)acetyl]amino]-6-[(1R,2R)-1,2,3-trihydroxypropyl]oxane-2-carboxylic acid
Canonical SMILES
C[C@H]([C@@H](C(=O)O)N)O[C@@H]1[C@@H]([C@H]([C@H]([C@H](O1)CO[C@@]2(C[C@@H]([C@H]([C@@H](O2)[C@@H]([C@@H](CO)O)O)NC(=O)CNC(=O)OCCOC)O)C(=O)O)O)O)NC(=O)C
InChI
InChI=1S/C27H46N4O19/c1-10(16(28)23(40)41)48-24-18(30-11(2)33)21(39)20(38)14(49-24)9-47-27(25(42)43)6-12(34)17(22(50-27)19(37)13(35)8-32)31-15(36)7-29-26(44)46-5-4-45-3/h10,12-14,16-22,24,32,34-35,37-39H,4-9,28H2,1-3H3,(H,29,44)(H,30,33)(H,31,36)(H,40,41)(H,42,43)/t10-,12+,13-,14-,16+,17-,18-,19-,20+,21-,22-,24+,27-/m1/s1
InChIKey
GAQMWPRWVIGRRV-IVDGIBIRSA-N
Cross-matching ID
PubChem CID
70683024
DrugBank ID
DB00019
TTD ID
D0AT8C
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Granulocyte colony-stimulating factor receptor (G-CSF-R) TTC70AJ CSF3R_HUMAN Binder [12]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Central nervous system neoplasm
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Granulocyte colony-stimulating factor receptor (G-CSF-R) DTT CSF3R 2.08E-08 0.36 0.96
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Pegfilgrastim (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Cladribine DM3JDRP Major Additive immunosuppressive effects by the combination of Pegfilgrastim and Cladribine. Mature B-cell leukaemia [2A82] [13]

References

1 Pegfilgrastim-induced hyperleukocytosis. Ann Pharmacother. 2007 Sep;41(9):1524-30.
2 A standard database for drug repositioning. Sci Data. 2017 Mar 14;4:170029.
3 Feasibility and efficacy of low-dose pegfilgrastim for CD34(+) cell mobilization in lymphoma. J Clin Apher. 2020 Sep;35(5):413-419.
4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6969).
5 Efficacy and safety of second-line therapy of docetaxel plus ramucirumab after first-line platinum-based chemotherapy plus immune checkpoint inhibitors in non-small cell lung cancer (SCORPION): a multicenter, open-label, single-arm, phase 2 trial. EClinicalMedicine. 2023 Nov 10;66:102303.
6 Effectiveness of biosimilar pegfilgrastim in patients with multiple myeloma after high-dose melphalan and autologous stem cell transplantation. Ann Hematol. 2023 Jul;102(7):1915-1925.
7 Evaluating the safety and effectiveness of PegaGen(?) (pegfilgrastim) for the prevention of chemotherapy-induced febrile neutropenia: a post-marketing surveillance study. Support Care Cancer. 2022 Oct;30(10):8151-8158.
8 The clinical pharmacokinetics of escitalopram. Clin Pharmacokinet. 2007;46(4):281-90. doi: 10.2165/00003088-200746040-00002.
9 Neulasta (pegfilgrastim) - FDA Label
10 The design and development of pegfilgrastim (PEG-rmetHuG-CSF, Neulasta). Curr Pharm Des. 2004;10(11):1235-44. doi: 10.2174/1381612043452613.
11 pegfilgrastim | Cancer Care Ontario
12 Evidence that the granulocyte colony-stimulating factor (G-CSF) receptor plays a role in the pharmacokinetics of G-CSF and PegG-CSF using a G-CSF-R KO model. Pharmacol Res. 2004 Jul;50(1):55-8.
13 Cerner Multum, Inc. "UK Summary of Product Characteristics.".