cetrorelix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| gonadotropin-releasing-hormone (GnRH) inhibitors, peptides | 583 | 120287-85-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
LHRH antagonist
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.25 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 8 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 3 % | Benet LZ, Broccatelli F, Oprea TI |
| Vd (Volume of distribution) | 0.39 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.14 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 12 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 11, 2000 | FDA | EMD SERONO INC | |
| April 12, 1999 | EMA | MERCK EUROPE B.V. | |
| April 20, 2006 | PMDA | NIPPON KAYAKU CO., LTD. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 824.28 | 56.34 | 119 | 621 | 3895 | 63484387 |
| Premature ovulation | 149.80 | 56.34 | 15 | 725 | 7 | 63488275 |
| Blood luteinising hormone increased | 135.23 | 56.34 | 16 | 724 | 93 | 63488189 |
| Ascites | 95.46 | 56.34 | 30 | 710 | 40698 | 63447584 |
| Ovarian disorder | 60.77 | 56.34 | 10 | 730 | 720 | 63487562 |
| Abortion spontaneous | 60.02 | 56.34 | 22 | 718 | 47173 | 63441109 |
| Pelvic fluid collection | 58.95 | 56.34 | 10 | 730 | 866 | 63487416 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 852.41 | 67.81 | 114 | 474 | 3457 | 79740343 |
| Premature ovulation | 124.42 | 67.81 | 12 | 576 | 7 | 79743793 |
| Blood luteinising hormone increased | 95.53 | 67.81 | 12 | 576 | 199 | 79743601 |
| Ascites | 86.87 | 67.81 | 29 | 559 | 75533 | 79668267 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01CC02 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones |
| FDA PE | N0000008638 | Decreased GnRH Secretion |
| FDA MoA | N0000175084 | Gonadotropin Releasing Hormone Receptor Antagonists |
| MeSH PA | D005300 | Fertility Agents, Female |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D012102 | Reproductive Control Agents |
| FDA EPC | N0000175839 | Gonadotropin Releasing Hormone Receptor Antagonist |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:59229 | GnRH antagonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Prevention of premature ovulation during controlled ovarian stimulation | indication | 732970000 | |
| Premature Luteinizing Hormone Surges | indication | ||
| Prevention of premature ovulation | indication | ||
| Acute nephropathy | contraindication | 58574008 | |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.65 | acidic |
| pKa2 | 12.09 | acidic |
| pKa3 | 12.45 | acidic |
| pKa4 | 13.01 | acidic |
| pKa5 | 13.29 | acidic |
| pKa6 | 13.37 | acidic |
| pKa7 | 13.67 | acidic |
| pKa8 | 13.71 | acidic |
| pKa9 | 10.75 | Basic |
| pKa10 | 5.35 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.25MG BASE/VIAL | CETRORELIX ACETATE | TEVA PHARMS INC | A215737 | Aug. 12, 2022 | RX | POWDER | SUBCUTANEOUS | April 22, 2023 | COMPETITIVE GENERIC THERAPY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | GPCR | ANTAGONIST | Ki | 8.80 | CHEMBL | CHEMBL | |||
| Lutropin-choriogonadotropic hormone receptor | GPCR | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01685 | KEGG_DRUG |
| 130143-01-0 | SECONDARY_CAS_RN |
| 259338 | RXNORM |
| C0209366 | UMLSCUI |
| CHEBI:59224 | CHEBI |
| CHEMBL1200490 | ChEMBL_ID |
| CHEMBL2103735 | ChEMBL_ID |
| DB00050 | DRUGBANK_ID |
| C062876 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1190 | IUPHAR_LIGAND_ID |
| 6661 | INN_ID |
| OON1HFZ4BA | UNII |
| 25074887 | PUBCHEM_CID |
| 15671 | MMSL |
| 362200 | MMSL |
| 37942 | MMSL |
| d04706 | MMSL |
| 007799 | NDDF |
| 007800 | NDDF |
| 326083001 | SNOMEDCT_US |
| 395906005 | SNOMEDCT_US |
| 412114000 | SNOMEDCT_US |
| 4021277 | VANDF |
| 4024232 | VANDF |
Pharmaceutical products:
None