SB-743921 HYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C31H33ClN2O3.ClH
Molecular Weight	553.519
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CC(C)[C@@H](N(CCCN)C(=O)C1=CC=C(C)C=C1)C2=C(CC3=CC=CC=C3)C(=O)C4=C(O2)C=C(Cl)C=C4

InChI

InChIKey=MLMZVWABFOLFGV-LNLSOMNWSA-N

InChI=1S/C31H33ClN2O3.ClH/c1-20(2)28(34(17-7-16-33)31(36)23-12-10-21(3)11-13-23)30-26(18-22-8-5-4-6-9-22)29(35)25-15-14-24(32)19-27(25)37-30;/h4-6,8-15,19-20,28H,7,16-18,33H2,1-3H3;1H/t28-;/m1./s1

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	C31H33ClN2O3
Molecular Weight	517.058
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25860245
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23875972 | https://clinicaltrials.gov/ct2/show/NCT00136513 | https://www.ncbi.nlm.nih.gov/pubmed/20461380

SB-743921 is a synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits the ATP-binding domain of the kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. SB-743921 has greater than 40,000 fold selectivity for KSP over other kinesins. SB-743921 has demonstrated promising anti-cancer activity in a variety of in vivo and in vitro human cancer models in preclinical studies. Furthermore, anti-cancer effect has been demonstrated in taxane-refractory malignancies with SB-743921. Toxicity studies demonstrated predictable neutropenias and gastrointestinal toxicities without clear evidence of neurotoxicity. The recommended phase II dose for SB-743921 as a 1-h infusion every 21 days is 4 mg/m2.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Kinesin-like protein 1 12 Target ID: CHEMBL4581 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23875972	Inhibitor 8504		0.14 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Large B-cell lymphoma 3 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25860245	Primary	Preclinical	Unknown Approved Use Unknown
Solid tumors 147 Sources: https://clinicaltrials.gov/ct2/show/NCT00136513	Primary	Phase I 438	Unknown Approved Use Unknown
Non-Hodgkin's lymphoma 81 Sources: https://clinicaltrials.gov/ct2/show/NCT00343564	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
233 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	2 mg/m² single, intravenous dose: 2 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
489 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	4 mg/m² single, intravenous dose: 4 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
607 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
817 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	6 mg/m² single, intravenous dose: 6 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
803 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	8 mg/m² single, intravenous dose: 8 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1706 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	2 mg/m² single, intravenous dose: 2 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3776 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	4 mg/m² single, intravenous dose: 4 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3776 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3776 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	6 mg/m² single, intravenous dose: 6 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3776 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	8 mg/m² single, intravenous dose: 8 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
31.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	2 mg/m² single, intravenous dose: 2 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
28 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	4 mg/m² single, intravenous dose: 4 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
36.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	5 mg/m² single, intravenous dose: 5 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
33.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	6 mg/m² single, intravenous dose: 6 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
30.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20461380/	8 mg/m² single, intravenous dose: 8 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered:	SB743921 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	DLT: Thrombocytopenia, Dehydration... Other AEs: Neutropenia, Fatigue... Dose limiting toxicities: Thrombocytopenia (grade 3-4, 57%) Dehydration (grade 3, 14%) Other AEs: Neutropenia (grade 3-4, 57%) Fatigue (grade 1-2, 57%) Leucopenia (grade 3-4, 14%) Nausea (grade 1-2, 14%) Anemia (grade 3-4, 29%) Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
4 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	DLT: Hypophosphatemia, Pulmonary embolism... Dose limiting toxicities: Hypophosphatemia (grade 3, 3.7%) Pulmonary embolism (grade 5, 3.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	DLT: Sepsis... Other AEs: Neutropenia, Thrombocytopenia... Dose limiting toxicities: Sepsis (grade 4, 10%) Other AEs: Neutropenia (grade 3-4, 40%) Thrombocytopenia (grade 1-2, 10%) Fatigue (grade 1-2, 10%) Pyrexia (grade 1-2, 10%) Dyspnea (grade 1-2, 10%) Leucopenia (grade 3-4, 20%) Nausea (grade 1-2, 30%) Anemia (grade 1-2, 40%) Cough (grade 1-2, 10%) Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	DLT: Neutropenia... Other AEs: Thrombocytopenia, Fatigue... Dose limiting toxicities: Neutropenia (grade 3-4, 57%) Other AEs: Thrombocytopenia (grade 1-4, 29%) Fatigue (grade 1-2, 14%) Pyrexia (grade 1-2, 29%) Leucopenia (grade 1-2, 29%) Nausea (grade 1-2, 29%) Anemia (grade 3-4, 14%) Diarrhea (grade 1-2, 14%) Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	DLT: Febrile neutropenia... Dose limiting toxicities: Febrile neutropenia (grade 4, 33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
6 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 6 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	DLT: Neutropenia, Hyponatremia... Dose limiting toxicities: Neutropenia (grade 4, 33.3%) Hyponatremia (grade 3, 33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
8 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 8 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	DLT: Neutropenia, Transaminase elevation... Dose limiting toxicities: Neutropenia (grade 4, 33.3%) Transaminase elevation (grade 3-4, 33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/

AEs

Overview

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

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDIzMjU0MjkifX0=	no [IC50 >25 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDIzMjU0MjkifX0=	no [IC50 >25 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDIzMjU0MjkifX0=	no [IC50 >25 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjMyNTQyOSJ9fQ==	no [IC50 >25 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjMyNTQyOSJ9fQ==	yes [IC50 4 uM]

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjMyNTQyOSJ9fQ==

PubMed

Title	Date	PubMed
The novel kinesin spindle protein (KSP) inhibitor SB-743921 exhibits marked activity in in vivo and in vitro models of aggressive large B-cell lymphoma.	2015	25860245

Patents

Sample Use Guides

In Vivo Use Guide

The recommended phase II dose for SB-743921 as a 1-h infusion every 21 days is 4 mg/m2 .

Route of Administration: Intravenous

In Vitro Use Guide

For in vitro assays, cells were counted and resuspended at a concentration of 3 x105 cells / well in a 24-well plate. SB-743921 was diluted in IMDM medium with 10% fetal bovine serum. Concentrations of SB-743921 from 1 nM to 10 μM were used in most assays. In pulse chase experiments cells were preincubated with SB-743921 for 1 or 3 hours. The cells were then washed twice with phosphate buffer solution 1X (PBS 1X) and resuspended in IMDM medium with 10% FBS. The cells were then incubated for 24, 48, or 72 hours prior to recording luminescence.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 21:05:17 GMT 2025` Edited by `admin` on `Tue Apr 01 21:05:17 GMT 2025`
Record UNII	2YW6FB68GM
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

BENZAMIDE, N-(3-AMINOPROPYL)-N-((1R)-1-(7-CHLORO-4-OXO-3-(PHENYLMETHYL)-4H-1-BENZOPYRAN-2-YL)-2-METHYLPROPYL)-4-METHYL-, HYDROCHLORIDE (1:1)

Preferred Name

English

SB-743921 HYDROCHLORIDE

Code

English

Code System Code Type Description

CAS

940929-33-9

Created by admin on Tue Apr 01 21:05:17 GMT 2025 , Edited by admin on Tue Apr 01 21:05:17 GMT 2025

PRIMARY

FDA UNII

2YW6FB68GM

Created by admin on Tue Apr 01 21:05:17 GMT 2025 , Edited by admin on Tue Apr 01 21:05:17 GMT 2025

PRIMARY

PUBCHEM

49867937

Created by admin on Tue Apr 01 21:05:17 GMT 2025 , Edited by admin on Tue Apr 01 21:05:17 GMT 2025

PRIMARY

EPA CompTox

DTXSID80678822

Created by admin on Tue Apr 01 21:05:17 GMT 2025 , Edited by admin on Tue Apr 01 21:05:17 GMT 2025

PRIMARY

Related Record Type Details


					511W07DGWZ

SB-743921 HYDROCHLORIDE MONOHYDRATE

SOLVATE->ANHYDROUS


					24DSZ1VN92

SB-743921

PARENT -> SALT/SOLVATE

Amount:

Related Record Type Details


					24DSZ1VN92

SB-743921

ACTIVE MOIETY

Amount:

AE	Significance	Dose	Population
Nausea	grade 1-2, 14%	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Fatigue	grade 1-2, 57%	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Dehydration	grade 3, 14% DLT	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Leucopenia	grade 3-4, 14%	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Anemia	grade 3-4, 29%	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Neutropenia	grade 3-4, 57%	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Thrombocytopenia	grade 3-4, 57% DLT	10 mg/m2 1 times / 2 weeks multiple, intravenous Highest studied dose Dose: 10 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 10 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Hypophosphatemia	grade 3, 3.7% DLT	4 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Pulmonary embolism	grade 5, 3.7% DLT	4 mg/m2 1 times / 3 weeks multiple, intravenous MTD Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Cough	grade 1-2, 10%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Dyspnea	grade 1-2, 10%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Fatigue	grade 1-2, 10%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Pyrexia	grade 1-2, 10%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Thrombocytopenia	grade 1-2, 10%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Nausea	grade 1-2, 30%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Anemia	grade 1-2, 40%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Leucopenia	grade 3-4, 20%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Neutropenia	grade 3-4, 40%	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Sepsis	grade 4, 10% DLT	6 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 6 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Diarrhea	grade 1-2, 14%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Fatigue	grade 1-2, 14%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Leucopenia	grade 1-2, 29%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Nausea	grade 1-2, 29%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Pyrexia	grade 1-2, 29%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Thrombocytopenia	grade 1-4, 29%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Anemia	grade 3-4, 14%	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Neutropenia	grade 3-4, 57% DLT	9 mg/m2 1 times / 2 weeks multiple, intravenous MTD Dose: 9 mg/m2, 1 times / 2 weeks Route: intravenous Route: multiple Dose: 9 mg/m2, 1 times / 2 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/25665464/
Febrile neutropenia	grade 4, 33.3% DLT	5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 5 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Hyponatremia	grade 3, 33.3% DLT	6 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 6 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Neutropenia	grade 4, 33.3% DLT	6 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 6 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 6 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Transaminase elevation	grade 3-4, 33.3% DLT	8 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 8 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/
Neutropenia	grade 4, 33.3% DLT	8 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 8 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 8 mg/m2, 1 times / 3 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20461380/

Details

SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/25860245Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23875972 | https://clinicaltrials.gov/ct2/show/NCT00136513 | https://www.ncbi.nlm.nih.gov/pubmed/20461380

Originator

Approval Year

Targets

Conditions

Approved Use

Approved Use

Approved Use

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Tox targets

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25860245
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23875972 | https://clinicaltrials.gov/ct2/show/NCT00136513 | https://www.ncbi.nlm.nih.gov/pubmed/20461380

C_max

T_1/2

Drug as perpetrator