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Drug ReportsMethylnaltrexone
Relistor(methylnaltrexone)
Relistor (methylnaltrexone) is a small molecule pharmaceutical. Methylnaltrexone was first approved as Relistor on 2008-04-24. It is used to treat constipation in the USA. It has been approved in Europe to treat constipation and opioid-related disorders. The pharmaceutical is active against mu-type opioid receptor. In addition, it is known to target kappa-type opioid receptor and delta-type opioid receptor.
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Commercial
Clinical
Drug
Target
Variants
Financial
Trends
Safety
Events Timeline
5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
signs and symptoms pathological conditionsD013568
chemically-induced disordersD064419
mental disordersD001523
Trade Name
FDA
EMA
Relistor
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Methylnaltrexone bromide
Tradename
Company
Number
Date
Products
RELISTORSalix PharmaceuticalsN-208271 RX2016-07-19
1 products, RLD, RS
RELISTORSalix PharmaceuticalsN-021964 RX2008-04-24
3 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
relistorNew Drug Application2024-05-14
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
Expires
Flag
FDA Information
Methylnaltrexone Bromide, Relistor, Salix
85242762031-03-10DP
89566512031-03-10DP
93144612031-03-10DP
103074172031-03-10DP
103765052031-03-10DP
84206632029-09-30U-1185
91801252029-09-30DPU-1185
94924452029-09-30DPU-1185
97243432029-09-30DPU-1185
Methylnaltrexone Bromide, Relistor, Salix Pharms
82474252030-12-31U-1185
88224902029-09-30DPU-1185
85520252024-04-08DP
96690962024-04-08DP
103765842024-04-08DPU-1185
ATC Codes
A: Alimentary tract and metabolism drugs
— A06: Drugs for constipation
— A06A: Drugs for constipation
— A06AH: Peripheral opioid receptor antagonists
— A06AH01: Methylnaltrexone bromide
HCPCS
Code
Description
J2212
Injection, methylnaltrexone, 0.1 mg
Clinical
Clinical Trials
59 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
ConstipationD003248HP_0002019K59.0—487321
Opioid-induced constipationD000079689———474216
GastroparesisD018589EFO_1000948K31.84—1—1—2
Velopharyngeal insufficiencyD014681HP_0000220————2—2
St elevation myocardial infarctionD000072657—————1—1
Morphine dependenceD009021EFO_0005612————1—1
Coronary artery diseaseD003324—I25.1———1—1
ParalysisD010243HP_0003470————1—1
Esophageal motility disordersD015154—K22.4———1—1
Esophageal diseasesD004935EFO_0009544K22.9———1—1
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Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
IleusD045823———22——4
Pancreatic neoplasmsD010190EFO_0003860C25—12——2
Intestinal diseasesD007410HP_0002242K63.9—11——2
Ventral herniaD006555EFO_1001866K43——1——1
HerniaD006547HP_0100790K40-K46——1——1
PancreatitisD010195HP_0001733K85—11——1
Enteral nutritionD004750————1——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients———41———5
NeoplasmsD009369—C8011———2
Gastrointestinal diseasesD005767———1———1
Opioid-related disordersD009293EFO_0005611F11—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Intestinal obstructionD007415—K56.602————2
Liver diseasesD008107HP_0002910K70-K771————1
Renal insufficiencyD051437HP_0000083N191————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
HypersensitivityD006967HP_0012393T78.40————11
Chronic painD059350HP_0012532—————11
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameMethylnaltrexone
INNmethylnaltrexone bromide
Description
Methylnaltrexone is a member of phenanthrenes.
Classification
Small molecule
Drug classnarcotic agonists/antagonists (normorphine type)
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
C[N+]1(CC2CC2)CC[C@]23c4c5ccc(O)c4O[C@H]2C(=O)CC[C@@]3(O)[C@H]1C5
Identifiers
PDB—
CAS-ID83387-25-1
RxCUI—
ChEMBL IDCHEMBL1186579
ChEBI ID—
PubChem CID5361918
DrugBankDB06800
UNII IDRFO6IL3D3M (ChemIDplus, GSRS)
Target
Agency Approved
OPRM1
OPRM1
Organism
Homo sapiens
Gene name
OPRM1
Gene synonyms
MOR1
NCBI Gene ID
Protein name
mu-type opioid receptor
Protein synonyms
hMOP, MOP, Mu opiate receptor, Mu opioid receptor, mu opioid receptor hMOR-1a
Uniprot ID
Mouse ortholog
Oprm1 (18390)
mu-type opioid receptor (Q9R1M0)
Alternate
OPRK1
OPRK1
OPRD1
OPRD1
Organism
Homo sapiens
Gene name
OPRK1
Gene synonyms
OPRK
NCBI Gene ID
Protein name
kappa-type opioid receptor
Protein synonyms
kappa opioid receptor, Opiate receptor, kappa-1
Uniprot ID
Mouse ortholog
Oprk1 (18387)
kappa-type opioid receptor (P33534)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 869 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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1,045 adverse events reported
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