relugolix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
gonadotropin releasing hormone (GnRH) antagonists 5432 737789-87-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • relugolix
  • TAK-385
  • orgovyx
  • relumina
  • RVT 601
Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone.
  • Molecular weight: 623.64
  • Formula: C29H27F2N7O5S
  • CLOGP: 3.16
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 2
  • TPSA: 129.23
  • ALOGS: -5.50
  • ROTB: 9
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.12 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.04 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.781 Moderate 0.76
caco2-efflux Caco-2 efflux ratio (BA/AB) 14.622 Moderate 0.76
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.194 10^-6 cm/s Moderate 0.76
dh-clint Dog hepatocyte intrinsic clearance 4.634 uL/min/10^6 cells Moderate 0.76
dppb Dog plasma protein binding (% unbound) 30.440 % Moderate 0.76
fcs-ppb Fetal calf serum protein binding (% unbound) 46.610 % Moderate 0.76
herg hERG pIC50 5.095 pIC50 Moderate 0.76
hh-clint Human hepatocyte intrinsic clearance 10.740 uL/min/10^6 cells Moderate 0.76
hlm-clint Human liver microsomal intrinsic clearance 52 uL/min/mg protein Moderate 0.76
hppb Human plasma protein binding (% unbound) 24.240 % Moderate 0.76
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,IKBKB,ITK,KDR,KIT,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 47
kinase-selectivity-class ACVR2B,AXL,CDK9,DDR1,EIF2AK3,ERBB2,FLT3,GRK2,MAP3K21,MAPK7,PDK1,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,SIK2,SIK3,STK33,TEK 21
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 26.485 Moderate 0.76
mh-clint Mouse hepatocyte intrinsic clearance 59.841 Moderate 0.76
mppb Mouse plasma protein binding (% unbound) 17.050 Moderate 0.76
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 37.757 Moderate 0.76
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 43.980 % Moderate 0.76
rh-clint Rat hepatocyte intrinsic clearance 35.481 uL/min/10^6 cells Moderate 0.76
rh-fuinc Rat hepatocyte fraction unbound in incubation 57.770 % Moderate 0.76
rppb Rat plasma protein binding (% unbound) 19.970 % Moderate 0.76
solubility-dd Solubility at pH 7.4 in DMSO 18.923 uM Moderate 0.76

Approvals:

DateAgencyCompanyOrphan
Aug. 1, 2019 PMDA Takeda Pharmaceutical Company Limited
Dec. 18, 2020 FDA MYOVANT SCIENCES
July 16, 2021 EMA Gedeon Richter Plc.

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
Genital haemorrhage 103.67 83.05 17 138 8685 90619607
Intermenstrual bleeding 102.69 83.05 17 138 9206 90619086

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
Therapy interrupted 1031.02 33.57 254 2983 21996 42596102
Hot flush 596.06 33.57 165 3072 22186 42595912
Fatigue 177.30 33.57 189 3048 435452 42182646
Prostatic specific antigen increased 113.03 33.57 44 3193 16881 42601217
Incorrect dose administered 112.12 33.57 62 3175 52912 42565186
Death 107.25 33.57 153 3084 471032 42147066
Incorrect dosage administered 85.90 33.57 21 3216 1697 42616401
Blood testosterone increased 77.56 33.57 19 3218 1548 42616550
Blood testosterone abnormal 61.25 33.57 13 3224 556 42617542
Prostatic specific antigen abnormal 34.77 33.57 9 3228 915 42617183
Dizziness 34.45 33.57 65 3172 249189 42368909

FDA Adverse Event Reporting System (Geriatric)

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
Hot flush 490.12 32.53 138 2395 65898 110520868
Therapy interrupted 382.25 32.53 107 2426 49715 110537051
Fatigue 140.44 32.53 154 2379 1215804 109370962
Prostatic specific antigen increased 128.90 32.53 34 2499 12477 110574289
Incorrect dose administered 114.49 32.53 53 2480 103588 110483178
Death 96.93 32.53 98 2435 698771 109887995
Uterine myoma expulsion 58.11 32.53 6 2527 0 110586766
Incorrect dosage administered 56.83 32.53 14 2519 3904 110582862
Intermenstrual bleeding 53.42 32.53 15 2518 6919 110579847
Genital haemorrhage 48.28 32.53 14 2519 7238 110579528
Asthenia 37.67 32.53 61 2472 688938 109897828
Metastases to bone 34.41 32.53 16 2517 31356 110555410
Blood testosterone abnormal 33.95 32.53 6 2527 331 110586435

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H01CC54 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
HYPOTHALAMIC HORMONES
Anti-gonadotropin-releasing hormones
ATC L02BX04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Other hormone antagonists and related agents
FDA PE N0000008638 Decreased GnRH Secretion
FDA MoA N0000175084 Gonadotropin Releasing Hormone Receptor Antagonists
MeSH PA D000726 Androgen Antagonists
MeSH PA D006727 Hormone Antagonists
FDA EPC N0000175839 Gonadotropin Releasing Hormone Receptor Antagonist
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187064 Cytochrome P450 2B6 Inducers
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190118 Cytochrome P450 3A Inducers
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

H01CC Anti-gonadotropin-releasing hormones 6 drugs
cetrorelixelagolixestradiolganirelixlinzagolixnorethisterone
L02BX Other hormone antagonists and related agents 3 drugs
abarelixabiraterone acetatedegarelix

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Lower abdominal pain indication 54586004
Uterine fibroids indication 95315005 DOID:13223
Pain associated with endometriosis indication 129103003
Menorrhagia indication 386692008
Malignant tumor of prostate indication 399068003 DOID:10283
Abnormal uterine bleeding due to uterine fibroid indication 16754891000119106




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 10449191 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 10786501 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 11583526 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 12097198 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 12144809 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER, MODIFIED BY DOSE-SEPARATING ADMINISTRATIONS OF RELUGOLIX AND A P-GP INHIBITOR, WHEN CO-ADMINISTRATION OF RELUGOLIX AND THE P-GP INHIBITOR IS UNAVOIDABLE
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 12336990 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG ORGOVYX SUMITOMO PHARMA AM N214621 Dec. 18, 2020 RX TABLET ORAL 12629370 Sept. 29, 2037 TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
1MG;0.5MG;40MG MYFEMBREE SUMITOMO PHARMA AM N214846 May 26, 2021 RX TABLET ORAL 11033551 Sept. 29, 2037 MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) IN PREMENOPAUSAL WOMEN
1MG;0.5MG;40MG MYFEMBREE SUMITOMO PHARMA AM N214846 May 26, 2021 RX TABLET ORAL 11957684 Sept. 29, 2037 MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) IN PREMENOPAUSAL WOMEN
1MG;0.5MG;40MG MYFEMBREE SUMITOMO PHARMA AM N214846 May 26, 2021 RX TABLET ORAL 11793812 May 3, 2038 MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1MG;0.5MG;40MG MYFEMBREE SUMITOMO PHARMA AM N214846 May 26, 2021 RX TABLET ORAL Jan. 27, 2026 INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF MVT-601-035

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR ANTAGONIST IC50 9.92 SCIENTIFIC LITERATURE DRUG LABEL
Gonadotropin-releasing hormone receptor GPCR ANTAGONIST IC50 9.48 IUPHAR

External reference:

IDSource
D10888 KEGG_DRUG
P76B05O5V6 UNII
C3896936 UMLSCUI
CHEBI:750198 CHEBI
CHEMBL1800159 ChEMBL_ID
10348973 PUBCHEM_CID
DB11853 DRUGBANK_ID
9628 INN_ID
C561634 MESH_SUPPLEMENTAL_RECORD_UI
5586 IUPHAR_LIGAND_ID
1144477009 SNOMEDCT_US
1144510001 SNOMEDCT_US
4039939 VANDF
342118 MMSL
39104 MMSL
d09698 MMSL
018596 NDDF
2472778 RXNORM
P76B05O5V6 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Orgovyx HUMAN PRESCRIPTION DRUG LABEL 1 72974-120 TABLET, FILM COATED 120 mg ORAL NDA 30 sections
Orgovyx HUMAN PRESCRIPTION DRUG LABEL 1 72974-120 TABLET, FILM COATED 120 mg ORAL NDA 30 sections
Myfembree HUMAN PRESCRIPTION DRUG LABEL 3 72974-415 TABLET, FILM COATED 40 mg ORAL NDA 30 sections