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cridanimod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| immunomodulators, both stimulant/suppressive and stimulant | 4853 | 38609-97-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A small molecule that can increase progesterone receptor (PR) expression, with potential antineoplastic adjuvant activity. Upon intramuscular administration, cridanimod is able to induce the expression of PR in endometrial cancer. This could increase the sensitivity of endometrial cancer cells to progestin monotherapy. In combination with a progestin, cancer cells could be eradicated through increased PR-mediated signaling, leading to an inhibition of luteinizing hormone (LH) release from the pituitary gland, via a negative feedback mechanism, and, eventually, an inhibition of estrogen release from the ovaries. This leads to an inhibition of cellular growth in estrogen-dependent tumor cells. In addition, this agent is able to increase the production and release of interferon (IFN) alpha and beta. PR is often downregulated in endometrial cancer and makes it resistant to progestin-mediated hormone therapy.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.451 | High | 0.81 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 5.741 | High | 0.81 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.957 | 10^-6 cm/s | High | 0.81 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.059 | uL/min/10^6 cells | High | 0.81 |
| dppb | Dog plasma protein binding (% unbound) | 14.180 | % | High | 0.81 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 16.890 | % | High | 0.81 |
| herg | hERG pIC50 | 4.497 | pIC50 | High | 0.81 |
| hh-clint | Human hepatocyte intrinsic clearance | 0.769 | uL/min/10^6 cells | High | 0.81 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.090 | uL/min/mg protein | High | 0.81 |
| hppb | Human plasma protein binding (% unbound) | 7.330 | % | High | 0.81 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK1,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 66 | |||
| kinase-selectivity-class | AXL,EIF2AK3 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.050 | High | 0.81 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 1.102 | High | 0.81 | |
| mppb | Mouse plasma protein binding (% unbound) | 15.100 | High | 0.81 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.662 | High | 0.81 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.890 | % | High | 0.81 |
| rh-clint | Rat hepatocyte intrinsic clearance | 0.820 | uL/min/10^6 cells | High | 0.81 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.210 | % | High | 0.81 |
| rppb | Rat plasma protein binding (% unbound) | 7.550 | % | High | 0.81 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 914.113 | uM | High | 0.81 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L03AX18 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSTIMULANTS IMMUNOSTIMULANTS Other immunostimulants |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L03AX Other immunostimulants 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.63 | acidic |
| pKa2 | 1.78 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Trypsin | Enzyme | AC50 | 5.15 | CHEMBL | |||||
| Stimulator of interferon genes protein | Membrane receptor | Kd | 5.48 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10507 | KEGG_DRUG |
| CHEBI:136036 | CHEBI |
| CHEMBL1569545 | ChEMBL_ID |
| DB13674 | DRUGBANK_ID |
| C0044659 | UMLSCUI |
| 1K5 | PDB_CHEM_ID |
| 8018 | INN_ID |
| 38072 | PUBCHEM_CID |
| X91E9EME19 | UNII |
| C077681 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None