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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
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 Application, NDA authorized generic2020-04-01
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
constipationHP_0002019D003248K59.0
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
16 clinical trials
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Mock data
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Pre-eclampsiaD011225EFO_0000668O1412—316
Pregnancy-induced hypertensionD046110O13———213
Indications Phases 3
No data
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Type 1 diabetes mellitusD003922EFO_0001359E1011——13
HypertensionD006973EFO_0000537I1011——12
ProteinuriaD011507HP_0000093R8011———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Orthostatic intoleranceD0549712————2
Autonomic nervous system diseasesD001342EFO_0009532G901————1
Orthostatic hypotensionD007024I95.11————1
Healthy volunteers/patients—1————1
Postural orthostatic tachycardia syndromeD054972G90.A1————1
Chronic fatigue syndromeD015673EFO_0004540G93.311————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameMETHYLNALTREXONE
INNmethylnaltrexone bromide
Description
Methylnaltrexone (MNTX, brand name Relistor), used in form of methylnaltrexone bromide (INN, USAN, BAN), is a medication that acts as a peripherally acting μ-opioid receptor antagonist that acts to reverse some of the side effects of opioid drugs such as constipation without significantly affecting pain relief or precipitating withdrawals. Because MNTX is a quaternary ammonium cation, it cannot cross the blood–brain barrier, and so has antagonist effects throughout the body, counteracting effects such as itching and constipation, but without affecting opioid effects in the brain such as pain relief. However, since a significant fraction (up to 60%) of opioid analgesia can be mediated by opioid receptors on peripheral sensory neurons, particularly in inflammatory conditions such as arthritis, traumatic or surgical pain, MNTX may increase pain under such circumstances.
Classification
Small molecule
Drug classnarcotic agonists/antagonists (normorphine type)
Image (chem structure or protein)
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-ID73232-52-7
RxCUI—
ChEMBL IDCHEMBL1186579
ChEBI ID—
PubChem CID5361917
DrugBankDB06800
UNII IDRFO6IL3D3M (ChemIDplus, GSRS)
Target
Agency Approved
OPRM1
OPRM1
Organism
Homo sapiens
Gene name
OPRM1
Gene synonyms
MOR1
NCBI Gene ID
4988
Protein name
mu-type opioid receptor
Protein synonyms
hMOP, MOP, Mu opiate receptor, Mu opioid receptor, mu opioid receptor hMOR-1a
Uniprot ID
Q9UN57
Mouse ortholog
Oprm1 (18390)
mu-type opioid receptor (P42866)
Alternate
OPRK1
OPRK1
OPRD1
OPRD1
Organism
Homo sapiens
Gene name
OPRK1
Gene synonyms
OPRK
NCBI Gene ID
4986
Protein name
kappa-type opioid receptor
Protein synonyms
kappa opioid receptor, Opiate receptor, kappa-1
Uniprot ID
Q499G4
Mouse ortholog
Oprk1 (18387)
kappa-type opioid receptor (P33534)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
Mock data
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Additional graphs summarizing 783 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
Mock data
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446 adverse events reported
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