Details of the Drug

General Information of Drug (ID: DMUL45H)

• Drug Name: Naltrexone
• Synonyms: Depotrex; Naltrel; Vivitrex; Vivitrol; Naltrexone Depot; IBS therapy, Pain Therapeutics; Irritable bowel syndrome therapy, Pain Therapeutics; PTI-901; XR-NTX; Naltrexone (sustained release), DAS; Naltrexone (sustained release), elbion; Naltrexone depot (injectable suspension), DrugAbuse Sciences; Naltrexone depot (injectable suspension), elbion; Opioid antagonists (irritable bowel syndrome), Pain Therapeutics; Naltrexone (low-dose), Pain Therapeutics; Naltrexone (polymer microcapsule depot, opioid addiction/alcohol dependency), Biotek; Naltrexone (transdermal, alcohol/opioid dependence), Syntropharma; Naltrexone (once-monthly controlled-release, Medisorb), Alkermes

Indication

Disease Entry	ICD 11	Status	REF
Alcohol dependence	6C40.2	Approved	[1]
Chronic alcoholism	6C40.2Z	Approved	[2]
Crohn disease	DD70	Approved	[3]
Gastroparesis	DA41.00	Approved	[3]
Inflammatory bowel disease	DD72	Approved	[3]
Obesity	5B81	Approved	[3]
Ulcerative colitis	DD71	Approved	[3]
Human immunodeficiency virus infection	1C62	Phase 4	[4]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 2	[5]
Chronic pain	MG30	Investigative	[3]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 341.4
  Logarithm of the Partition Coefficient (xlogp); 1.9
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 5
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [6]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 57 mL/min/kg [7]
  Elimination: 1% of drug is excreted from urine in the unchanged form [6]
  Half-life: The concentration or amount of drug in body reduced by one-half in 1.9 hours [7]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.43935 micromolar/kg/day [8]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.79% [7]
  Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 7.6 L/kg [7]
  Water Solubility: The ability of drug to dissolve in water is measured as 100 mg/mL [6]
• Chemical Identifiers:
  Formula: C20H23NO4
  IUPAC Name: (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
  Canonical SMILES: C1CC1CN2CC[C@]34[C@@H]5C(=O)CC[C@]3([C@H]2CC6=C4C(=C(C=C6)O)O5)O
  InChI: InChI=1S/C20H23NO4/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11/h3-4,11,15,18,22,24H,1-2,5-10H2/t15-,18+,19+,20-/m1/s1
  InChIKey: DQCKKXVULJGBQN-XFWGSAIBSA-N
• Cross-matching ID:
  PubChem CID: 5360515
  ChEBI ID: CHEBI:7465
  CAS Number: 16590-41-3
  DrugBank ID: DB00704
  TTD ID: D0PG8O
  VARIDT ID: DR00968
  INTEDE ID: DR1128
  ACDINA ID: D00455
• 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
Opioid receptor (OPR)	TTN4QDT	NOUNIPROTAC	Antagonist	[9]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[10]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
D(2) dopamine receptor (DRD2)	OTBLXKEG	DRD2_HUMAN	Drug Response	[11]
Follitropin subunit beta (FSHB)	OTGLS283	FSHB_HUMAN	Gene/Protein Processing	[12]
Gamma-aminobutyric acid receptor subunit alpha-6 (GABRA6)	OTX4UC3O	GBRA6_HUMAN	Drug Response	[11]
Gamma-aminobutyric acid receptor subunit beta-2 (GABRB2)	OTAOZIGX	GBRB2_HUMAN	Drug Response	[11]
Lutropin subunit beta (LHB)	OT5GBOVJ	LSHB_HUMAN	Gene/Protein Processing	[12]
Mu-type opioid receptor (OPRM1)	OT16AAT8	OPRM_HUMAN	Drug Response	[9]
Nitric oxide synthase, inducible (NOS2)	OTKKIOJ1	NOS2_HUMAN	Gene/Protein Processing	[13]
Sodium-dependent dopamine transporter (SLC6A3)	OT39XG28	SC6A3_HUMAN	Drug Response	[14]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Naltrexone

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Disulfiram	DMCL2OK	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Disulfiram.	Substance abuse [6C40]	[15]

Coadministration of a Drug Treating the Disease Different from Naltrexone (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Remdesivir.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[16]
Tretinoin	DM49DUI	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tretinoin.	Acne vulgaris [ED80]	[15]
Isotretinoin	DM4QTBN	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Isotretinoin.	Acne vulgaris [ED80]	[15]
Nicotinamide	DMUPE07	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Nicotinamide.	Acquired cutaneous blood vessel malformation [EF20]	[15]
Pioglitazone	DMKJ485	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Pioglitazone.	Acute diabete complication [5A2Y]	[15]
Tagraxofusp	DM9HQ5U	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tagraxofusp.	Acute myeloid leukaemia [2A60]	[15]
Gilteritinib	DMTI0ZO	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Gilteritinib.	Acute myeloid leukaemia [2A60]	[15]
Inotersen	DMJ93CT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Inotersen.	Amyloidosis [5D00]	[15]
Dronedarone	DMA8FS5	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Dronedarone.	Angina pectoris [BA40]	[15]
Bedaquiline	DM3906J	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[17]
Oxymetholone	DMFXUT8	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Oxymetholone.	Aplastic anaemia [3A70]	[15]
Posaconazole	DMUL5EW	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Posaconazole.	Aspergillosis [1F20]	[15]
Zileuton	DMVRIC2	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Zileuton.	Asthma [CA23]	[15]
Clavulanate	DM2FGRT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Clavulanate.	Bacterial infection [1A00-1C4Z]	[15]
Clarithromycin	DM4M1SG	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Clarithromycin.	Bacterial infection [1A00-1C4Z]	[15]
Sulfamethoxazole	DMB08GE	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Sulfamethoxazole.	Bacterial infection [1A00-1C4Z]	[15]
Levofloxacin	DMS60RB	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Levofloxacin.	Bacterial infection [1A00-1C4Z]	[15]
Troleandomycin	DMUZNIG	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Troleandomycin.	Bacterial infection [1A00-1C4Z]	[15]
Minocycline	DMVN5OH	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Minocycline.	Bacterial infection [1A00-1C4Z]	[15]
Telithromycin	DMZ4P3A	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Telithromycin.	Bacterial infection [1A00-1C4Z]	[15]
Pexidartinib	DMS2J0Z	Major	Increased risk of hepatotoxicity by the combination of Naltrexone and Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[18]
Temozolomide	DMKECZD	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Temozolomide.	Brain cancer [2A00]	[15]
Lomustine	DMMWSUL	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lomustine.	Brain cancer [2A00]	[15]
Lapatinib	DM3BH1Y	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lapatinib.	Breast cancer [2C60-2C6Y]	[15]
LY2835219	DM93VBZ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and LY2835219.	Breast cancer [2C60-2C6Y]	[15]
Pralatrexate	DMAO80I	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Pralatrexate.	Breast cancer [2C60-2C6Y]	[15]
Tucatinib	DMBESUA	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tucatinib.	Breast cancer [2C60-2C6Y]	[15]
Bosutinib	DMTI8YE	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Bosutinib.	Breast cancer [2C60-2C6Y]	[15]
Trastuzumab Emtansine	DMU1LXS	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Trastuzumab Emtansine.	Breast cancer [2C60-2C6Y]	[15]
Fluoxymesterone	DMUHCF1	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fluoxymesterone.	Breast cancer [2C60-2C6Y]	[15]
Atorvastatin	DMF28YC	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Atorvastatin.	Cardiovascular disease [BA00-BE2Z]	[15]
Fenofibric acid	DMGO2MC	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fenofibric acid.	Cardiovascular disease [BA00-BE2Z]	[15]
Macitentan	DMP79A1	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Macitentan.	Cardiovascular disease [BA00-BE2Z]	[15]
Chenodiol	DMQ8JIK	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Chenodiol.	Cholelithiasis [DC11]	[15]
Phenylbutazone	DMAYL0T	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Phenylbutazone.	Chronic pain [MG30]	[15]
Ketoprofen	DMRKXPT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ketoprofen.	Chronic pain [MG30]	[15]
Regorafenib	DMHSY1I	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Regorafenib.	Colorectal cancer [2B91]	[15]
Intedanib	DMSTA36	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Intedanib.	Colorectal cancer [2B91]	[15]
Pasireotide	DMHM7JS	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Pasireotide.	Cushing syndrome [5A70]	[15]
Ivacaftor	DMZC1HS	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ivacaftor.	Cystic fibrosis [CA25]	[15]
Ethanol	DMDRQZU	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ethanol.	Cystitis [GC00]	[15]
Nefazodone	DM4ZS8M	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Nefazodone.	Depression [6A70-6A7Z]	[15]
Milnacipran	DMBFE74	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Milnacipran.	Depression [6A70-6A7Z]	[15]
Polatuzumab vedotin	DMF6Y0L	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Polatuzumab vedotin.	Diffuse large B-cell lymphoma [2A81]	[15]
Felbamate	DM1V5ZS	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Felbamate.	Epilepsy/seizure [8A61-8A6Z]	[15]
Fosphenytoin	DMOX3LB	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fosphenytoin.	Epilepsy/seizure [8A61-8A6Z]	[15]
Ethotoin	DMXWOCP	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ethotoin.	Epilepsy/seizure [8A61-8A6Z]	[15]
Cannabidiol	DM0659E	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Cannabidiol.	Epileptic encephalopathy [8A62]	[15]
Mefenamic acid	DMK7HFI	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Mefenamic acid.	Female pelvic pain [GA34]	[15]
Dantrolene	DM1D8XY	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Dantrolene.	Fever [MG26]	[15]
Itraconazole	DMCR1MV	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Itraconazole.	Fungal infection [1F29-1F2F]	[15]
Terbinafine	DMI6HUW	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Terbinafine.	Fungal infection [1F29-1F2F]	[15]
Ketoconazole	DMPZI3Q	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ketoconazole.	Fungal infection [1F29-1F2F]	[15]
Atovaquone	DMY4UMW	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Atovaquone.	Fungal infection [1F29-1F2F]	[15]
Sunitinib	DMCBJSR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Sunitinib.	Gastrointestinal stromal tumour [2B5B]	[15]
Lamivudine	DMI347A	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lamivudine.	Hepatitis virus infection [1E50-1E51]	[15]
177Lu-DOTATATE	DMT8GVU	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[15]
Isoniazid	DM5JVS3	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Isoniazid.	HIV-infected patients with tuberculosis [1B10-1B14]	[15]
Rifampin	DMA8J1G	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Rifampin.	HIV-infected patients with tuberculosis [1B10-1B14]	[15]
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[15]
Tipranavir	DM8HJX6	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tipranavir.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Emtricitabine	DMBMUWZ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Emtricitabine.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Zalcitabine	DMH7MUV	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Zalcitabine.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Didanosine	DMI2QPE	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Didanosine.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Rilpivirine	DMJ0QOW	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Abacavir	DMMN36E	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Abacavir.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Darunavir	DMN3GCH	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Darunavir.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Maraviroc	DMTL94F	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Maraviroc.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Fluvastatin	DM4MDJY	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fluvastatin.	Hyper-lipoproteinaemia [5C80]	[15]
Fenofibrate	DMFKXDY	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fenofibrate.	Hyper-lipoproteinaemia [5C80]	[15]
Mipomersen	DMGSRN1	Major	Increased risk of hepatotoxicity by the combination of Naltrexone and Mipomersen.	Hyper-lipoproteinaemia [5C80]	[19]
Rosuvastatin	DMMIQ7G	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Rosuvastatin.	Hyper-lipoproteinaemia [5C80]	[15]
Teriflunomide	DMQ2FKJ	Major	Increased risk of hepatotoxicity by the combination of Naltrexone and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[20]
BMS-201038	DMQTAGO	Major	Increased risk of hepatotoxicity by the combination of Naltrexone and BMS-201038.	Hyper-lipoproteinaemia [5C80]	[21]
Captopril	DM458UM	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Captopril.	Hypertension [BA00-BA04]	[15]
Methyldopa	DM5I621	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Methyldopa.	Hypertension [BA00-BA04]	[15]
Perindopril	DMOPZDT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Perindopril.	Hypertension [BA00-BA04]	[15]
Quinapril	DMR8H31	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Quinapril.	Hypertension [BA00-BA04]	[15]
Lisinopril	DMUOK4C	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lisinopril.	Hypertension [BA00-BA04]	[15]
Tolvaptan	DMIWFRL	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[15]
Bremelanotide	DM20LIM	Major	Altered absorption of Naltrexone due to GI dynamics variation caused by Bremelanotide.	Hypoactive sexual desire dysfunction [HA00]	[22]
Pirfenidone	DM6VZFQ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Pirfenidone.	Idiopathic interstitial pneumonitis [CB03]	[15]
Givosiran	DM5PFIJ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Givosiran.	Inborn porphyrin/heme metabolism error [5C58]	[15]
Febuxostat	DMDEXQ0	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Febuxostat.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[15]
Meclofenamic acid	DM05FXR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Meclofenamic acid.	Inflammatory spondyloarthritis [FA92]	[15]
Crizotinib	DM4F29C	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Crizotinib.	Lung cancer [2C25]	[15]
Ceritinib	DMB920Z	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ceritinib.	Lung cancer [2C25]	[15]
Lurbinectedin	DMEFRTZ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lurbinectedin.	Lung cancer [2C25]	[15]
Alectinib	DMP1I6Y	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Alectinib.	Lung cancer [2C25]	[15]
BIBW 2992	DMTKD7Q	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and BIBW 2992.	Lung cancer [2C25]	[15]
Pralsetinib	DMWU0I2	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Pralsetinib.	Lung cancer [2C25]	[15]
Capmatinib	DMYCXKL	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Capmatinib.	Lung cancer [2C25]	[15]
Sulphadoxine	DMZI2UF	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Sulphadoxine.	Malaria [1F40-1F45]	[15]
Inotuzumab ozogamicin	DMAC130	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[15]
Calaspargase pegol	DMQZBXI	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Calaspargase pegol.	Malignant haematopoietic neoplasm [2B33]	[15]
Idelalisib	DM602WT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Idelalisib.	Mature B-cell leukaemia [2A82]	[23]
IPI-145	DMWA24P	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and IPI-145.	Mature B-cell leukaemia [2A82]	[15]
Blinatumomab	DMGECIJ	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Blinatumomab.	Mature B-cell lymphoma [2A85]	[15]
Mercaptopurine	DMTM2IK	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Mercaptopurine.	Mature B-cell lymphoma [2A85]	[15]
Ponatinib	DMYGJQO	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ponatinib.	Mature B-cell lymphoma [2A85]	[15]
Cytarabine	DMZD5QR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Cytarabine.	Mature B-cell lymphoma [2A85]	[15]
Arry-162	DM1P6FR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Arry-162.	Melanoma [2C30]	[15]
Vemurafenib	DM62UG5	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Vemurafenib.	Melanoma [2C30]	[15]
Ipilimumab	DMJTIYK	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ipilimumab.	Melanoma [2C30]	[15]
Dacarbazine	DMNPZL4	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Dacarbazine.	Melanoma [2C30]	[15]
Danazol	DML8KTN	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Danazol.	Menstrual cycle bleeding disorder [GA20]	[15]
Exjade	DMHPRWG	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Exjade.	Mineral absorption/transport disorder [5C64]	[15]
Riluzole	DMECBWN	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Riluzole.	Motor neuron disease [8B60]	[15]
Carfilzomib	DM48K0X	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Carfilzomib.	Multiple myeloma [2A83]	[15]
Panobinostat	DM58WKG	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Panobinostat.	Multiple myeloma [2A83]	[15]
Elotuzumab	DMEYHG9	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Elotuzumab.	Multiple myeloma [2A83]	[15]
Tecfidera	DM2OVDT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tecfidera.	Multiple sclerosis [8A40]	[15]
Siponimod	DM2R86O	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Siponimod.	Multiple sclerosis [8A40]	[15]
Fingolimod	DM5JVAN	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fingolimod.	Multiple sclerosis [8A40]	[15]
Ozanimod	DMT6AM2	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ozanimod.	Multiple sclerosis [8A40]	[15]
Fedratinib	DM4ZBK6	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fedratinib.	Myeloproliferative neoplasm [2A20]	[15]
Nilotinib	DM7HXWT	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Nilotinib.	Myeloproliferative neoplasm [2A20]	[15]
Bupropion	DM5PCS7	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Bupropion.	Nicotine use disorder [6C4A]	[15]
Entrectinib	DMMPTLH	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Entrectinib.	Non-small cell lung cancer [2C25]	[15]
Orlistat	DMRJSP8	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Orlistat.	Obesity [5B80-5B81]	[15]
Etodolac	DM6WJO9	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Etodolac.	Pain [MG30-MG3Z]	[15]
Ibuprofen	DM8VCBE	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ibuprofen.	Pain [MG30-MG3Z]	[15]
Bromfenac	DMKB79O	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Bromfenac.	Postoperative inflammation [1A00-CA43]	[15]
ABIRATERONE	DM8V75C	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and ABIRATERONE.	Prostate cancer [2C82]	[15]
Bicalutamide	DMZMSPF	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Bicalutamide.	Prostate cancer [2C82]	[15]
Ambrisentan	DMD1QXW	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Ambrisentan.	Pulmonary hypertension [BB01]	[15]
Axitinib	DMGVH6N	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Axitinib.	Renal cell carcinoma [2C90]	[15]
Meloxicam	DM2AR7L	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Meloxicam.	Rheumatoid arthritis [FA20]	[15]
Tocilizumab	DM7J6OR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Tocilizumab.	Rheumatoid arthritis [FA20]	[15]
Oxaprozin	DM9UB0P	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Oxaprozin.	Rheumatoid arthritis [FA20]	[15]
Flurbiprofen	DMGN4BY	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Flurbiprofen.	Rheumatoid arthritis [FA20]	[15]
Sulfasalazine	DMICA9H	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Sulfasalazine.	Rheumatoid arthritis [FA20]	[15]
Sarilumab	DMOGNXY	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Sarilumab.	Rheumatoid arthritis [FA20]	[15]
Leflunomide	DMR8ONJ	Major	Increased risk of hepatotoxicity by the combination of Naltrexone and Leflunomide.	Rheumatoid arthritis [FA20]	[20]
Larotrectinib	DM26CQR	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Larotrectinib.	Solid tumour/cancer [2A00-2F9Z]	[15]
PDX-101	DM6OC53	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and PDX-101.	Solid tumour/cancer [2A00-2F9Z]	[15]
Trabectedin	DMG3Y89	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Trabectedin.	Solid tumour/cancer [2A00-2F9Z]	[15]
LEE011	DMMX75K	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[15]
Methyltestosterone	DMWLFGO	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Methyltestosterone.	Solid tumour/cancer [2A00-2F9Z]	[15]
Fostamatinib	DM6AUHV	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Fostamatinib.	Thrombocytopenia [3B64]	[15]
Eltrombopag	DMOGFIX	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Eltrombopag.	Thrombocytopenia [3B64]	[15]
Lenvatinib	DMB1IU4	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Lenvatinib.	Thyroid cancer [2D10]	[15]
Methimazole	DM25FL8	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Methimazole.	Thyrotoxicosis [5A02]	[15]
Trimetrexate	DMDEA85	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Trimetrexate.	Toxoplasmosis [1F57]	[15]
Elagolix	DMB2C0E	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Elagolix.	Uterine fibroid [2E86]	[15]
Amiodarone	DMUTEX3	Moderate	Increased risk of hepatotoxicity by the combination of Naltrexone and Amiodarone.	Ventricular tachyarrhythmia [BC71]	[15]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
Cysteine hydrochloride	E00318	25150	Antioxidant
D&C red no. 28	E00491	6097185	Colorant
Diethyl phthalate	E00135	6781	Plasticizing agent; Solvent
Erythrosine sodium anhydrous	E00324	27872	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Ascorbic acid	E00579	54670067	Acidulant; Antioxidant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Dibutyl sebacate	E00160	7986	Plasticizing agent
Edetate disodium	E00186	8759	Complexing agent
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Gelatin	E00630	Not Available	Other agent
Hydroxypropyl cellulose	E00632	Not Available	Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 400	E00653	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Saccharose	E00091	5988	Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium chloride	E00077	5234	Diluent; Tonicity agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Haematite red	E00236	14833	Colorant
Hydrophobic colloidal silica	E00285	24261	Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
Ethyl cellulose	E00699	Not Available	Coating agent; Microencapsulating agent; Binding agent; Diluent; Viscosity-controlling agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Naltrexone Hydrochloride 0.8mg extended release capsule	0.8mg	Extended Release Capsule	Oral
Naltrexone Hydrochloride 20mg extended release capsule	20mg	Extended Release Capsule	Oral
Naltrexone Hydrochloride 8mg extended release tablet	8mg	Extended Release Tablet	Oral
Naltrexone Hydrochloride 90mg extended release tablet	90mg	Extended Release Tablet	Oral
Naltrexone Hydrochloride 50mg tablet	50mg	Tablet	Oral
Naltrexone 50 mg tablet	50 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (ANDA) 074918.
• [3] Naltrexone FDA Label
• [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: 1639).
• [5] ClinicalTrials.gov (NCT04365985) Study of Immunomodulation Using Naltrexone and Ketamine for COVID-19. U.S. National Institutes of Health.
• [6] BDDCS applied to over 900 drugs
• [7] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [8] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [9] An evaluation of mu-opioid receptor (OPRM1) as a predictor of naltrexone response in the treatment of alcohol dependence: results from the Combined Pharmacotherapies and Behavioral Interventions for Alcohol Dependence (COMBINE) study. Arch Gen Psychiatry. 2008 Feb;65(2):135-44.
• [10] In vivo chronic exposure to heroin or naltrexone selectively inhibits liver microsome formation of estradiol-3-glucuronide in the rat. Biochem Pharmacol. 2008 Sep 1;76(5):672-9.
• [11] Predicting the effect of naltrexone and acamprosate in alcohol-dependent patients using genetic indicators. Addict Biol. 2009 Jul;14(3):328-37.
• [12] Chronic naltrexone treatment induces desensitization of the luteinizing hormone pulse generator for opioid blockade in hyperprolactinemic patients. J Clin Endocrinol Metab. 1995 May;80(5):1739-42. doi: 10.1210/jcem.80.5.7745028.
• [13] Low dose naltrexone therapy in multiple sclerosis. Med Hypotheses. 2005;64(4):721-4.
• [14] Association between the Stin2 VNTR polymorphism of the serotonin transporter gene and treatment outcome in alcohol-dependent patients. Alcohol Alcohol. 2008 Sep-Oct;43(5):516-22. doi: 10.1093/alcalc/agn048. Epub 2008 Jun 14.
• [15] Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
• [16] Cerner Multum, Inc. "Australian Product Information.".
• [17] Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
• [18] Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
• [19] Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
• [20] Canadian Pharmacists Association.
• [21] Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
• [22] Product Information. Vyleesi (bremelanotide). AMAG Pharmaceuticals Inc, Lexington, MA.
• [23] Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.