U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C23H28N8O4
Molecular Weight 480.5205
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of COPANLISIB

SMILES

COc1c(ccc2c1N=C(N=C(c3c[nH]c(=N)nc3)O)N4CCN=C24)OCCCN5CCOCC5

InChI

InChIKey=PZBCKZWLPGJMAO-UHFFFAOYSA-N
InChI=1S/C23H28N8O4/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15/h3-4,13-14H,2,5-12H2,1H3,(H2,24,26,27)(H,28,29,32)

HIDE SMILES / InChI

Molecular Formula C23H28N8O4
Molecular Weight 480.5205
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: http://www.selleckchem.com/products/bay80-6946.html

Copanlisib, developed by Bayer, is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Copanlisib is currently under Phase II/III clinical trials for the treatment of non-Hodgkin lymphoma and chronic lymphocytic leukemia.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ALIQOPA

Approved Use

ALIQOPA is indicated for the treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies. Accelerated approval was granted for this indication based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

Launch Date

1505260800000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
463 ng/mL
60 mg 1 times / week steady-state, intravenous
dose: 60 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
447 μg/L
0.8 mg/kg 1 times / week multiple, intravenous
dose: 0.8 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1570 ng × h/mL
60 mg 1 times / week steady-state, intravenous
dose: 60 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1280 μg × h/L
0.8 mg/kg 1 times / week multiple, intravenous
dose: 0.8 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
39.1 h
60 mg 1 times / week steady-state, intravenous
dose: 60 mg
route of administration: Intravenous
experiment type: STEADY-STATE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
35.6 h
0.8 mg/kg 1 times / week multiple, intravenous
dose: 0.8 mg/kg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
COPANLISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Doses

Doses

DosePopulationAdverse events​
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
DLT: Alanine aminotransferase increased, Aspartate aminotransferase increased...
Dose limiting toxicities:
Alanine aminotransferase increased (grade 3, 1 patient)
Aspartate aminotransferase increased (grade 4, 1 patient)
Acidosis lactic (grade 4, 1 patient)
Anion gap (grade 4, 1 patient)
Ketonaemia (grade 4, 1 patient)
Left ventricular systolic dysfunction (grade 3, 1 patient)
Sources:
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Disc. AE: Hyperglycemia, Neutropenia...
AEs leading to
discontinuation/dose reduction:
Hyperglycemia (7%)
Neutropenia (5%)
Hypertension (5%)
Pneumonitis (2%)
Hyperglycemia (2%)
Sources:
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Disc. AE: Thrombocytopenia, Neutropenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (3%)
Neutropenia (1.8%)
Anemia (1.2%)
Nausea (1.2%)
Fatigue (2.4%)
Hypercalcemia (1.2%)
Acute kidney injury (1.6%)
Pneumonitis (3.6%)
Febrile neutropenia (1.8%)
Diarrhea (2.4%)
Pyrexia (5.4%)
Sepsis (1.8%)
Hyperglycemia (4.8%)
Pneumonitis (6%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Alanine aminotransferase increased grade 3, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Left ventricular systolic dysfunction grade 3, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Acidosis lactic grade 4, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Anion gap grade 4, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Aspartate aminotransferase increased grade 4, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Ketonaemia grade 4, 1 patient
DLT, Disc. AE
1.2 mg/kg 3 times / month steady, intravenous
Highest studied dose
Dose: 1.2 mg/kg, 3 times / month
Route: intravenous
Route: steady
Dose: 1.2 mg/kg, 3 times / month
Sources:
unhealthy, 62 years (range: 35–86 years)
Health Status: unhealthy
Age Group: 62 years (range: 35–86 years)
Sex: M+F
Sources:
Hyperglycemia 2%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Pneumonitis 2%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Hypertension 5%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia 5%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Hyperglycemia 7%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anemia 1.2%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Hypercalcemia 1.2%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Nausea 1.2%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Acute kidney injury 1.6%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Febrile neutropenia 1.8%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Neutropenia 1.8%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Sepsis 1.8%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Diarrhea 2.4%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Fatigue 2.4%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Thrombocytopenia 3%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Pneumonitis 3.6%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Hyperglycemia 4.8%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Pyrexia 5.4%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Pneumonitis 6%
Disc. AE
60 mg 3 times / month steady, intravenous
Recommended|MTD
Dose: 60 mg, 3 times / month
Route: intravenous
Route: steady
Dose: 60 mg, 3 times / month
Sources:
unhealthy, adult
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 0.09 uM]
yes [IC50 10.8 uM]
yes [IC50 11.5 uM]
yes [IC50 7 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
yes
yes (co-administration study)
Comment: ole, a strong CYP3A inhibitor which is also with inhibitory activity against human transporter P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP), administered at a dose of 200 mg once daily for 10 days increased the mean AUC of a single IV dose of 60 mg ALIQOPA 53% with no effect on Cmax in patients with cancer
Page: 65
Tox targets

Tox targets

Sourcing
PubMed

PubMed

TitleDatePubMed
BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models.
2013 Nov
Preliminary results of a phase II study of single agent Bay 80-6946, a Novel PI3K inhibitor, in patients with relapsed/refractory, indolent or aggressive lymphoma.
2014 Feb
Patents

Sample Use Guides

60 mg in solution administered intravenously on Days 1, 8 and 15 of each 28-day treatment cycle
Route of Administration: Oral
Several breast cancer, endometrial cancer, and hematologic tumor cell lines were particularly sensitive to Copanlisib, with IC50 values less than 10nmol/L
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:29:59 UTC 2021
Edited
by admin
on Fri Jun 25 21:29:59 UTC 2021
Record UNII
WI6V529FZ9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
COPANLISIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
2-AMINO-N-(7-METHOXY-8-(3-(MORPHOLIN-4-YL)PROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL(PYRIMIDINE-5-CARBOXAMIDE
Common Name English
COPANLISIB [MI]
Common Name English
COPANLISIB [WHO-DD]
Common Name English
BAY-80-6946
Code English
2-AMINO-N-(7-METHOXY-8-(3-MORPHOLIN-4-YLPROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL)PYRIMIDINE-5-CARBOXAMIDE
Systematic Name English
BAY80-6946
Code English
COPANLISIB [INN]
Common Name English
5-PYRIMIDINECARBOXAMIDE, 2-AMINO-N-(2,3-DIHYDRO-7-METHOXY-8-(3-(4-MORPHOLINYL)PROPOXY)IMIDAZO(1,2-C)QUINAZOLIN-5-YL)-
Systematic Name English
BAY 80-6946
Code English
COPANLISIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 463314
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
WHO-ATC L01XX61
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 811321
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 552416
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
NCI_THESAURUS C2152
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 811421
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 552616
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
FDA ORPHAN DRUG 552516
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
EU-Orphan Drug EU/3/18/2064
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C96796
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
PUBCHEM
24989044
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
MERCK INDEX
M12036
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
WIKIPEDIA
Copanlisib
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
EVMPD
SUB184952
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
RXCUI
1945077
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
DRUG CENTRAL
5256
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL3218576
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
FDA UNII
WI6V529FZ9
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
CAS
1032568-63-0
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
LACTMED
Copanlisib
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
INN
9726
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
DRUG BANK
DB12483
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
EPA CompTox
1032568-63-0
Created by admin on Fri Jun 25 21:29:59 UTC 2021 , Edited by admin on Fri Jun 25 21:29:59 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
<10% OF METABOLISM
MINOR
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
90% OF METABOLISM
MAJOR
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
IC50
BINDER->LIGAND
BINDING
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
Related Record Type Details
METABOLITE -> PARENT
(DEALKYLATION BY CYP3A4), The six healthy male volunteers received a single i.v. infusion of 12 mg copanlisib (2.76 MBq (14C)copanlisib) in a total volume of 40 mL as a 1-h infusion in the morning, 1-h after a light breakfast. 5 Caucasians and 1 Asian with an age 54.8 +/- 5.2 yeas (mean +/- SD, range: 47-61 years) and a BMI of 24.8 kg/m^2. Non-smokers and reported at the most light alcohol use.
AMOUNT EXCRETED
FECAL; URINE
METABOLITE -> PARENT
(DEALKYLATION BY CYP3A4), The six healthy male volunteers received a single i.v. infusion of 12 mg copanlisib (2.76 MBq (14C)copanlisib) in a total volume of 40 mL as a 1-h infusion in the morning, 1-h after a light breakfast. 5 Caucasians and 1 Asian with an age 54.8 +/- 5.2 yeas (mean +/- SD, range: 47-61 years) and a BMI of 24.8 kg/m^2. Non-smokers and reported at the most light alcohol use.
AMOUNT EXCRETED
FECAL; URINE
METABOLITE -> PARENT
(DEALKYLATION BY CYP3A4), The six healthy male volunteers received a single i.v. infusion of 12 mg copanlisib (2.76 MBq (14C)copanlisib) in a total volume of 40 mL as a 1-h infusion in the morning, 1-h after a light breakfast. 5 Caucasians and 1 Asian with an age 54.8 +/- 5.2 yeas (mean +/- SD, range: 47-61 years) and a BMI of 24.8 kg/m^2. Non-smokers and reported at the most light alcohol use.
AMOUNT EXCRETED
FECAL; URINE
METABOLITE -> PARENT
(DEALKYLATION BY CYP3A4), The six healthy male volunteers received a single i.v. infusion of 12 mg copanlisib (2.76 MBq (14C)copanlisib) in a total volume of 40 mL as a 1-h infusion in the morning, 1-h after a light breakfast. 5 Caucasians and 1 Asian with an age 54.8 +/- 5.2 yeas (mean +/- SD, range: 47-61 years) and a BMI of 24.8 kg/m^2. Non-smokers and reported at the most light alcohol use.
AMOUNT EXCRETED
FECAL; URINE
Related Record Type Details
ACTIVE MOIETY
The six healthy male volunteers received a single i.v. infusion of 12 mg copanlisib (2.76 MBq (14C)copanlisib) in a total volume of 40 mL as a 1-h infusion in the morning, 1-h after a light breakfast. 5 Caucasians and 1 Asian with an age 54.8 +/- 5.2 yeas (mean +/- SD, range: 47-61 years) and a BMI of 24.8 kg/m^2. Non-smokers and reported at the most light alcohol use.
AMOUNT EXCRETED
FECAL; PLASMA; URINE
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC