TOMIVOSERTIB HYDROCHLORIDE

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H20N6O2.ClH
Molecular Weight	376.841
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CC1=C2N(C(=O)C(NC3=CC(N)=NC=N3)=C1)C4(CCCCC4)NC2=O

InChI

InChIKey=WBGPPUUXCGKTSC-UHFFFAOYSA-N

InChI=1S/C17H20N6O2.ClH/c1-10-7-11(21-13-8-12(18)19-9-20-13)16(25)23-14(10)15(24)22-17(23)5-3-2-4-6-17;/h7-9H,2-6H2,1H3,(H,22,24)(H3,18,19,20,21);1H

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

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

Molecular Formula	C17H20N6O2
Molecular Weight	340.3797
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29526098 | https://effector.com/pipeline/ | https://www.ncbi.nlm.nih.gov/pubmed/30459229

Tomivosertib (eFT-508) is a dual inhibitor of MAP kinase-interacting kinases (MNK1 and MNK2) thereby controlling translation. It has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors. Tomivosertib acts on multiple points in the cancer immunity cycle simultaneously, underscoring its therapeutic potential as both a monotherapy and in combination with existing checkpoint inhibitor treatments. Preclinical studies suggest combining tomivosertib with a checkpoint inhibitor can overcome mechanisms of resistance to checkpoint inhibitors, resulting in enhanced sensitivity to checkpoint inhibitors and a higher response rate. In addition, preclinical data demonstrate that tomivosertib as a single agent promotes antitumor immunity that persists after stopping drug treatment. Tomivosertib is currently being evaluated in Phase 2 clinical trials in solid tumors and lymphoma. Additionally, tomivosertib may be a new therapeutic for neuropathic pain.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
MAP kinase-interacting serine/threonine-protein kinase 1 2 Target ID: Q9BUB5 Gene ID: 8569.0 Gene Symbol: MKNK1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29526098	Inhibitor 8504		2.4 nM [IC50]
MAP kinase-interacting serine/threonine-protein kinase 2 2 Target ID: Q9HBH9 Gene ID: 2872.0 Gene Symbol: MKNK2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29526098	Inhibitor 8504		2.4 nM [IC50]

C_max

Value	Dose	Analyte	Population
0.11 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.24 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.3 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.37 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.54 μg/mL CLINICAL TRIAL https://web.archive.org/web/20221014202421/https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.46 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.15 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.23 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.46 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.4 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.49 μg/mL CLINICAL TRIAL https://web.archive.org/web/20221014202421/https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.58 μg/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1.5 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.3 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.6 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.7 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.8 μg × h/mL CLINICAL TRIAL https://web.archive.org/web/20221014202421/https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.6 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.98 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.3 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.6 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.1 μg × h/mL CLINICAL TRIAL https://web.archive.org/web/20221014202421/https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.5 μg × h/mL CLINICAL TRIAL https://effector.com/wp-content/uploads/eFFECTOR-eFT508-0001-ASCO-2017_final.pdf	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
9.7 h CLINICAL TRIAL https://www.sciencedirect.com/science/article/pii/S0006497119851406	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:		EFT-508 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

PubMed

Title	Date	PubMed
Nociceptor Translational Profiling Reveals the Ragulator-Rag GTPase Complex as a Critical Generator of Neuropathic Pain.	2019-01-16	30459229
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.	2018-04-26	29526098
Mitogen-activated Protein Kinase (MAPK) Interacting Kinases 1 and 2 (MNK1 and MNK2) as Targets for Cancer Therapy: Recent Progress in the Development of MNK Inhibitors.	2017	28164761

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:07:44 GMT 2025` Edited by `admin` on `Mon Mar 31 23:07:44 GMT 2025`
Record UNII	BW3S40K2UM
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SPIRO(CYCLOHEXANE-1,3'(2'H)-IMIDAZO(1,5-A)PYRIDINE)-1',5'-DIONE, 6'-((6-AMINO-4-PYRIMIDINYL)AMINO)-8'-METHYL-, HYDROCHLORIDE (1:1)

Preferred Name

English

TOMIVOSERTIB HYDROCHLORIDE

Official Name

English

EFT508HCL

Code

English

TOMIVOSERTIB HYDROCHLORIDE [USAN]

Common Name

English

EFT-508 HYDROCHLORIDE

Code

English

6'-((6-AMINOPYRIMIDIN-4-YL)AMINO)-8'-METHYL-2'HSPIRO(CYCLOHEXANE-1,3'-IMIDAZO(1,5-A)PYRIDINE)-1',5'-DIONE HYDROCHLORIDE

Systematic Name

English

Code System Code Type Description

CAS

1849590-02-8