romiplostim Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
colony stimulating factors 4996 267639-76-9

Description:

MoleculeDescription

Synonyms:

  • romiplostim
  • nplate
  • AMG-531
  • AMG531
Romiplostim, a member of the TPO mimetic class, is an Fc-peptide fusion protein (peptibody) that activates intracellular transcriptional pathways leading to increased platelet production via the TPO receptor (also known as cMpl). The peptibody molecule contains two identical single-chain subunits, each consisting of human immunoglobulin IgG1 Fc domain, covalently linked at the C-terminus to a peptide containing two thrombopoietin receptor-binding domains. Romiplostim has no amino acid sequence homology to endogenous TPO. Romiplostim is produced by recombinant DNA technology in Escherichia coli.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
30 mcg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 21, 2011 PMDA Kyowa Hakko Kirin
Aug. 22, 2008 FDA AMGEN
Feb. 4, 2009 EMA

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
Platelet count abnormal 1745.13 20.32 332 11264 2646 53334824
Platelet count decreased 1268.05 20.32 565 11031 107534 53229936
Therapeutic response decreased 1142.25 20.32 417 11179 47152 53290318
Thrombocytopenia 600.48 20.32 373 11223 138354 53199116
Thrombocytosis 452.71 20.32 124 11472 5408 53332062
Platelet count increased 282.18 20.32 112 11484 15695 53321775
Splenectomy 274.34 20.32 53 11543 456 53337014
Petechiae 258.99 20.32 101 11495 13504 53323966
Myelofibrosis 234.74 20.32 55 11541 1259 53336211
Drug ineffective 230.25 20.32 528 11068 816717 52520753
Biopsy bone marrow abnormal 209.97 20.32 39 11557 265 53337205
Haemorrhage 198.37 20.32 135 11461 57852 53279618
Bone marrow reticulin fibrosis 195.65 20.32 33 11563 116 53337354
Immune thrombocytopenia 186.45 20.32 72 11524 9366 53328104
Myelodysplastic syndrome 135.22 20.32 68 11528 16592 53320878
Death 133.31 20.32 260 11336 356972 52980498
Purpura 120.68 20.32 55 11541 10798 53326672
Deep vein thrombosis 100.17 20.32 106 11490 82807 53254663
Contusion 97.26 20.32 120 11476 110612 53226858
Hospitalisation 95.18 20.32 96 11500 70916 53266554
Off label use 93.05 20.32 268 11328 471944 52865526
Epistaxis 90.46 20.32 92 11504 68618 53268852
Mucosal haemorrhage 73.29 20.32 20 11576 856 53336614
Chronic lymphocytic leukaemia 73.22 20.32 27 11569 3089 53334381
Gingival bleeding 68.23 20.32 39 11557 12269 53325201
Vaginal haemorrhage 65.50 20.32 51 11545 26790 53310680
Rheumatoid arthritis 56.17 20.32 3 11593 314528 53022942
Bone marrow disorder 52.92 20.32 19 11577 2014 53335456
Therapy non-responder 52.64 20.32 59 11537 49061 53288409
Haematological malignancy 51.13 20.32 11 11585 168 53337302
Aplastic anaemia 47.82 20.32 27 11569 8294 53329176
Mouth haemorrhage 47.82 20.32 25 11571 6601 53330869
Pulmonary embolism 46.97 20.32 87 11509 114355 53223115
Ecchymosis 43.08 20.32 28 11568 11071 53326399
Drug hypersensitivity 40.55 20.32 5 11591 265237 53072233
Melaena 40.11 20.32 40 11556 29089 53308381
Leukocytosis 39.79 20.32 37 11559 24697 53312773
Headache 37.96 20.32 222 11374 536599 52800871
Leukoerythroblastic anaemia 35.37 20.32 6 11590 22 53337448
Acute myeloid leukaemia 34.57 20.32 29 11567 16903 53320567
Thrombosis 33.90 20.32 53 11543 60740 53276730
Toxicity to various agents 33.90 20.32 4 11592 219594 53117876
Rectal haemorrhage 33.24 20.32 43 11553 41438 53296032
White blood cell count increased 31.07 20.32 44 11552 46201 53291269
Platelet disorder 30.62 20.32 12 11584 1619 53335851
Cerebral haemorrhage 30.37 20.32 35 11561 29961 53307509
Cerebral venous thrombosis 29.63 20.32 13 11583 2331 53335139
Reticulin increased 26.97 20.32 4 11592 4 53337466
Embolism arterial 26.80 20.32 10 11586 1181 53336289
Sudden hearing loss 26.32 20.32 10 11586 1242 53336228
Blood blister 26.27 20.32 11 11585 1760 53335710
Rash maculo-papular 25.67 20.32 32 11564 29717 53307753
Diarrhoea 25.52 20.32 62 11534 625484 52711986
Haemorrhage intracranial 25.48 20.32 22 11574 13330 53324140
Cerebral venous sinus thrombosis 25.24 20.32 11 11585 1941 53335529
Marrow hyperplasia 25.20 20.32 8 11588 582 53336888
Portal vein thrombosis 25.16 20.32 12 11584 2607 53334863
Chronic myelomonocytic leukaemia 24.91 20.32 7 11589 334 53337136
Joint swelling 24.78 20.32 10 11586 234628 53102842
Nausea 22.92 20.32 86 11510 756005 52581465
Antibody test 22.58 20.32 4 11592 20 53337450
Megaloblasts increased 22.30 20.32 3 11593 0 53337470
Blood smear test abnormal 22.16 20.32 5 11591 96 53337374
Splenomegaly 21.56 20.32 18 11578 10421 53327049
Bone pain 21.33 20.32 39 11557 50683 53286787

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
Platelet count abnormal 1010.67 19.77 219 10005 2355 32500947
Therapeutic response decreased 845.28 19.77 314 9910 25606 32477696
Platelet count decreased 735.86 19.77 452 9772 114139 32389163
Drug ineffective 392.84 19.77 536 9688 382941 32120361
Bone marrow reticulin fibrosis 311.31 19.77 53 10171 122 32503180
Thrombocytosis 264.49 19.77 81 10143 3604 32499698
Platelet count increased 257.63 19.77 100 10124 9101 32494201
Thrombocytopenia 249.70 19.77 268 9956 148031 32355271
Myelodysplastic syndrome 208.54 19.77 109 10115 19929 32483373
Immune thrombocytopenia 164.77 19.77 71 10153 8426 32494876
Myelofibrosis 155.72 19.77 45 10179 1632 32501670
Haematological malignancy 147.28 19.77 30 10194 230 32503072
Splenectomy 143.79 19.77 32 10192 389 32502913
Hospitalisation 132.11 19.77 115 10109 48856 32454446
Petechiae 132.00 19.77 63 10161 9475 32493827
Coombs positive haemolytic anaemia 126.83 19.77 33 10191 802 32502500
Biopsy bone marrow abnormal 124.98 19.77 27 10197 283 32503019
Lymphadenitis 101.51 19.77 33 10191 1782 32501520
Death 94.21 19.77 298 9926 382219 32121083
Therapeutic product effect decreased 90.01 19.77 76 10148 30941 32472361
Deep vein thrombosis 79.51 19.77 99 10125 63614 32439688
Off label use 78.31 19.77 242 9982 306078 32197224
Haemolysis 77.29 19.77 41 10183 7700 32495602
Haemorrhage 76.88 19.77 86 10138 49362 32453940
Chronic lymphocytic leukaemia 76.00 19.77 35 10189 4850 32498452
Acute myeloid leukaemia 68.34 19.77 53 10171 19121 32484181
Epistaxis 59.05 19.77 80 10144 55775 32447527
Migraine 57.24 19.77 42 10182 13943 32489359
Investigation 52.75 19.77 17 10207 892 32502410
Gingival bleeding 50.68 19.77 30 10194 6951 32496351
Contusion 48.24 19.77 56 10168 33412 32469890
Drug interaction 48.18 19.77 6 10218 218179 32285123
Embolism arterial 46.77 19.77 14 10210 574 32502728
Therapy non-responder 44.34 19.77 53 10171 32601 32470701
Ecchymosis 43.53 19.77 27 10197 6801 32496501
Toxicity to various agents 41.56 19.77 4 10220 178037 32325265
Cellulitis gangrenous 41.01 19.77 10 10214 185 32503117
Bone marrow disorder 39.32 19.77 16 10208 1642 32501660
Pulmonary embolism 38.83 19.77 83 10141 83576 32419726
Platelet disorder 35.28 19.77 14 10210 1346 32501956
Mouth haemorrhage 33.96 19.77 21 10203 5260 32498042
Evans syndrome 32.64 19.77 9 10215 274 32503028
Thrombosis 31.89 19.77 54 10170 45700 32457602
Diarrhoea 30.77 19.77 42 10182 364760 32138542
Mesenteric vascular insufficiency 29.72 19.77 7 10217 111 32503191
Marrow hyperplasia 27.68 19.77 11 10213 1061 32502241
Embolism 27.51 19.77 21 10203 7393 32495909
Cerebrovascular accident 27.47 19.77 74 10150 86246 32417056
Myeloproliferative neoplasm 26.79 19.77 9 10215 538 32502764
Lymphoma 26.35 19.77 24 10200 10776 32492526
Non-Hodgkin's lymphoma 25.68 19.77 12 10212 1718 32501584
Vomiting 23.15 19.77 24 10200 235533 32267769
Multimorbidity 22.50 19.77 8 10216 567 32502735
Protein-losing gastroenteropathy 22.36 19.77 7 10217 334 32502968
Leukocytosis 22.36 19.77 32 10192 23435 32479867
White blood cell count increased 21.44 19.77 43 10181 41359 32461943
Therapeutic response delayed 21.35 19.77 7 10217 388 32502914
Platelet morphology abnormal 21.27 19.77 4 10220 19 32503283
Bone pain 21.25 19.77 29 10195 20315 32482987
Reticulin increased 21.20 19.77 3 10221 0 32503302
Acute kidney injury 20.71 19.77 38 10186 293430 32209872
Neutralising antibodies positive 20.69 19.77 5 10219 89 32503213
Blood blister 20.38 19.77 10 10214 1594 32501708
Mucosal haemorrhage 20.32 19.77 10 10214 1604 32501698
Hypotension 20.14 19.77 23 10201 216087 32287215

Pharmacologic Action:

SourceCodeDescription
ATC B02BX04 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
VITAMIN K AND OTHER HEMOSTATICS
Other systemic hemostatics
FDA MoA N0000175968 Thrombopoietin Receptor Agonists
FDA PE N0000175969 Increased Megakaryocyte Maturation
FDA PE N0000175970 Increased Platelet Production
FDA EPC N0000175973 Thrombopoietin Receptor Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic idiopathic thrombocytopenic purpura indication 13172003
Aplastic anemia indication 306058006 DOID:12449

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Thrombopoietin receptor Membrane receptor AGONIST DRUG LABEL DRUG LABEL

External reference:

IDSource
D08990 KEGG_DRUG
4028106 VUID
N0000177934 NUI
4028106 VANDF
CHEMBL1201832 ChEMBL_ID
C488777 MESH_SUPPLEMENTAL_RECORD_UI
6974 IUPHAR_LIGAND_ID
8587 INN_ID
DB05332 DRUGBANK_ID
GN5XU2DXKV UNII
135449332 PUBCHEM_CID
805452 RXNORM
147787 MMSL
25808 MMSL
d07320 MMSL
012794 NDDF
439122000 SNOMEDCT_US
441077008 SNOMEDCT_US
C2364481 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Nplate HUMAN PRESCRIPTION DRUG LABEL 1 55513-221 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 ug SUBCUTANEOUS BLA 28 sections
Nplate HUMAN PRESCRIPTION DRUG LABEL 1 55513-222 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 ug SUBCUTANEOUS BLA 28 sections
Nplate HUMAN PRESCRIPTION DRUG LABEL 1 55513-223 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 125 ug SUBCUTANEOUS BLA 28 sections