NAVOXIMOD PHOSPHATE

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H21FN2O2.H3O4P
Molecular Weight	414.3651
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OP(O)(O)=O.O[C@H](C[C@@H]1N2C=NC=C2C3=CC=CC(F)=C13)[C@H]4CC[C@H](O)CC4

InChI

InChIKey=GJKNKBNFVIDKPJ-HJFTWMQOSA-N

InChI=1S/C18H21FN2O2.H3O4P/c19-14-3-1-2-13-16-9-20-10-21(16)15(18(13)14)8-17(23)11-4-6-12(22)7-5-11;1-5(2,3)4/h1-3,9-12,15,17,22-23H,4-8H2;(H3,1,2,3,4)/t11-,12-,15-,17+;/m0./s1

HIDE SMILES / InChI

Molecular Formula	H3O4P
Molecular Weight	97.9952
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C18H21FN2O2
Molecular Weight	316.3699
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://adisinsight.springer.com/drugs/800039434 | https://www.ncbi.nlm.nih.gov/pubmed/30770348 | http://cancerres.aacrjournals.org/content/73/8_Supplement/491 | https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C113793https://www.ncbi.nlm.nih.gov/pubmed/26642377
Curator's Comment: description was created based on several sources, including https://www.google.com/patents/WO2012142237A8

NLG919 is a novel small-molecule IDO-pathway inhibitor. NLG919 potently inhibits this pathway in vitro and in cell-based assays. It is orally bioavailable and has a favorable pharmacokinetic and toxicity profile. In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ∼ 50%. Using IDO-expressing human monocyte-derived DCs in allogeneic MLR reactions, NLG919 potently blocked IDO-induced T cell suppression and restored robust T cell responses with an ED50=80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro. In vivo, in mice bearing large established B16F10 tumors, administration of NLG919 markedly enhanced the anti-tumor responses of naïve, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Indoleamine 2,3-dioxygenase 20 Target ID: CHEMBL4685 Sources: https://www.ncbi.nlm.nih.gov/pubmed/29247038	Inhibitor 8504		28.0 nM [IC50]
Indoleamine 2,3-dioxygenase 1 2 Target ID: CHEMBL1075294 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26642377	Inhibitor 8504		38.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cancer 609 Sources: https://www.google.com/patents/WO2012142237A8	Primary		Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
0.743 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
3.19 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
0.906 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
8.61 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
15 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
33.9 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1.26 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
3.71 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1.41 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
11.2 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
11.1 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
45.1 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	800 mg 2 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
1.48 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4.6 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
2.48 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
16.2 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
26.9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
54.3 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
3.08 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	50 mg 2 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
6.42 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	100 mg 2 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
5.49 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
21.9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
29 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
113 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	800 mg 2 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
5.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
11.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
10.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
9.13 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
10.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
17.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29921320/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	NAVOXIMOD plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

Doses

Dose	Population	Adverse events
800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	DLT: Diarrhea, Hypotension... Disc. AE: AST increased, ALT increased... Dose limiting toxicities: Diarrhea (grade 1, 16.7%) Hypotension (grade 3-4, 16.7%) Gastrointestinal hemorrhage (grade 4, 16.7%) AEs leading to discontinuation/dose reduction: AST increased (grade 2, 16.7%) ALT increased (grade 2, 16.7%) Maculopapular rash (grade 2, 16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/

AEs

AE	Significance	Dose	Population
Diarrhea	grade 1, 16.7% DLT	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/
ALT increased	grade 2, 16.7% Disc. AE	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/
AST increased	grade 2, 16.7% Disc. AE	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/
Maculopapular rash	grade 2, 16.7% Disc. AE	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/
Hypotension	grade 3-4, 16.7% DLT	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/
Gastrointestinal hemorrhage	grade 4, 16.7% DLT	800 mg 2 times / day multiple, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/29921320/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 inhibitor 2252	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C8 1057 CYP2B6 926 CYP2C19 2057 CYP1A2 2153	P-gp 2052 UGT2B7 456 UGT1A9 423

Drug as perpetrator

Target	Modality	Activity
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzk4OTk1MSJ9fQ==	moderate [IC50 5.7 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM5ODk5NTEifX0=	no [IC50 >100 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw0NzI5IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM5ODk5NTEifX0=	no [IC50 >100 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM5ODk5NTEifX0=	no [IC50 >100 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNzIxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM5ODk5NTEifX0=	no [IC50 >100 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM5ODk5NTEifX0=	no [IC50 >100 uM]
CYP3A4 2633	inducer 1966 Sources: https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.9b00662	unlikely
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzk4OTk1MSJ9fQ==	weak [IC50 86 uM]

Drug as victim

Target	Modality	Activity
UGT1A9 423	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/30973970/	major
UGT2B7 456	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/30973970/	major
P-gp 2052	substrate 4014 Sources: https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.9b00662	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzk4OTk1MSJ9fQ==

PubMed

Title	Date	PubMed
Phase I study of the indoleamine 2,3-dioxygenase 1 inhibitor navoximod (GDC-0919) as monotherapy and in combination with the PD-L1 inhibitor atezolizumab in Japanese patients with advanced solid tumours.	2020-04	31124055
Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor.	2019-08	30973970
Phase I Study of the Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Navoximod (GDC-0919) Administered with PD-L1 Inhibitor (Atezolizumab) in Advanced Solid Tumors.	2019-06-01	30770348
Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors.	2018-06-20	29921320
Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1.	2016-01-14	26642377

Patents

Sample Use Guides

In Vivo Use Guide

Recurrent/advanced solid tumors: administered as 50-800 mg BID on a 21/28 day and at 600 mg on a 28/28 day schedule. Navoximod was well-tolerated at doses up to 800 mg BID decreasing plasma kynurenine levels consistent with its half-life.

Route of Administration: Oral

In Vitro Use Guide

Navoximod is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 16:40:33 GMT 2025` Edited by `admin` on `Tue Apr 01 16:40:33 GMT 2025`
Record UNII	X3G215LI0R
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NAVOXIMOD PHOSPHATE

Common Name

English

5H-IMIDAZO(5,1-A)ISINDOLE-5-ETHANOL, 6-FLUORO-.ALPHA.-(TRANS-4-HYDROXYCYCLOHEXYL)-, (.ALPHA.R,5S)-, PHOSPHATE (1:1)

Preferred Name

English

Code System Code Type Description

PUBCHEM

121488180

Created by admin on Tue Apr 01 16:40:33 GMT 2025 , Edited by admin on Tue Apr 01 16:40:33 GMT 2025

PRIMARY

CAS

1793075-63-4

Created by admin on Tue Apr 01 16:40:33 GMT 2025 , Edited by admin on Tue Apr 01 16:40:33 GMT 2025

PRIMARY

FDA UNII

X3G215LI0R

Created by admin on Tue Apr 01 16:40:33 GMT 2025 , Edited by admin on Tue Apr 01 16:40:33 GMT 2025

PRIMARY

SMS_ID

300000013069

Created by admin on Tue Apr 01 16:40:33 GMT 2025 , Edited by admin on Tue Apr 01 16:40:33 GMT 2025

PRIMARY

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NAVOXIMOD

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					926SHL95NC

NAVOXIMOD

ACTIVE MOIETY

Details

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Approved Use

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator