Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H22F3N5O2S |
Molecular Weight | 441.47 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(SC(NC(=O)N2CCC[C@H]2C(N)=O)=N1)C3=CC=NC(=C3)C(C)(C)C(F)(F)F
InChI
InChIKey=STUWGJZDJHPWGZ-LBPRGKRZSA-N
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1
Molecular Formula | C19H22F3N5O2S |
Molecular Weight | 441.47 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/26793003
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26793003
Alpelisib (BYL719) is a PI3Kα-selective inhibitor. PI3K-AKT-mTOR pathway is frequently activated in cancer, therefore investigational PI3K inhibitor alpelisib is considered to be effective as an anticancer agent and has been in clinical development by Novartis. Alpelisib have demonstrated activity in preclinical models of solid tumors and had favorable tolerability profiles, with the most common adverse events consistent with “on-target” inhibition of PI3K in early clinical studies. There are ongoing clinical trials of alpelisib in a range of cancer types, including breast cancer, head and neck squamous cell carcinoma, non-small cell lung carcinoma, lymphoma, and glioblastoma multiforme. Combination therapy with other chemo therapeutics may be preferable.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=23726034
Curator's Comment: # Novartis
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P42336 Gene ID: 5290.0 Gene Symbol: PIK3CA Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27126994 |
5.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2480 ng/mL |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ALPELISIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
33224 ng × h/mL |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ALPELISIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.5 h |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ALPELISIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11% |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ALPELISIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg 1 times / day steady, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 48.0 years (range: 24-72 years) n = 7 Health Status: unhealthy Age Group: 48.0 years (range: 24-72 years) Sex: M+F Population Size: 7 Sources: |
DLT: Maculopapular rash, Conjunctivitis... Dose limiting toxicities: Maculopapular rash (grade 3, 2 patients) Sources: Conjunctivitis (grade 2, 1 patient) |
350 mg 1 times / day steady, oral Studied dose Dose: 350 mg, 1 times / day Route: oral Route: steady Dose: 350 mg, 1 times / day Sources: |
unhealthy, 54.5 years (range: 31-72 years) n = 8 Health Status: unhealthy Age Group: 54.5 years (range: 31-72 years) Sex: M+F Population Size: 8 Sources: |
DLT: Tumor infection... Dose limiting toxicities: Tumor infection (grade 4, 1 patient) Sources: |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Disc. AE: Hyperglycemia, Rash... AEs leading to discontinuation/dose reduction: Hyperglycemia (grade 3-4, 4.2%) Sources: Page: p. 138Rash (grade 3-4, 1.1%) Diarrhea (grade 3-4, 0.4%) Fatigue (grade 3-4, 1.1%) Nausea (grade 3-4, 0.4%) Hyperglycaemia (grade 3-4, 31.3%) Diarrhoea (grade 3-4, 5.6%) Rash (grade 3-4, 9.2%) Rash maculo-papular (grade 3-4, 8.8%) Stomatitis (grade 3-4, 2.1%) Mucosal inflammation (grade 3-4, 1.4%) Nausea (grade 3-4, 1.4%) Lipase increased (grade 3-4, 3.5%) Pyrexia (grade 3-4, 0.7%) Fatigue (grade 3-4, 1.4%) Pruritus (grade 3-4, 0.4%) Vomiting (grade 3-4, 0.4%) Asthenia (grade 3-4, 1.1%) Decreased appetite (grade 3-4, 0.4%) Alanine aminotransferase increased (grade 3-4, 2.1%) |
450 mg 1 times / day steady, oral Highest studied dose Dose: 450 mg, 1 times / day Route: oral Route: steady Dose: 450 mg, 1 times / day Sources: Page: p. 68 |
unhealthy Health Status: unhealthy Condition: advanced solid malignancies Sources: Page: p. 68 |
|
400 mg 1 times / day steady, oral MTD Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: Page: p. 76, 87 |
unhealthy n = 33 Health Status: unhealthy Condition: advanced solid malignancies Population Size: 33 Sources: Page: p. 76, 87 |
Sources: Page: p. 76, 87 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Conjunctivitis | grade 2, 1 patient DLT |
400 mg 1 times / day steady, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 48.0 years (range: 24-72 years) n = 7 Health Status: unhealthy Age Group: 48.0 years (range: 24-72 years) Sex: M+F Population Size: 7 Sources: |
Maculopapular rash | grade 3, 2 patients DLT |
400 mg 1 times / day steady, oral Studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 48.0 years (range: 24-72 years) n = 7 Health Status: unhealthy Age Group: 48.0 years (range: 24-72 years) Sex: M+F Population Size: 7 Sources: |
Tumor infection | grade 4, 1 patient DLT |
350 mg 1 times / day steady, oral Studied dose Dose: 350 mg, 1 times / day Route: oral Route: steady Dose: 350 mg, 1 times / day Sources: |
unhealthy, 54.5 years (range: 31-72 years) n = 8 Health Status: unhealthy Age Group: 54.5 years (range: 31-72 years) Sex: M+F Population Size: 8 Sources: |
Decreased appetite | grade 3-4, 0.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Diarrhea | grade 3-4, 0.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Nausea | grade 3-4, 0.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Pruritus | grade 3-4, 0.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Vomiting | grade 3-4, 0.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Pyrexia | grade 3-4, 0.7% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Asthenia | grade 3-4, 1.1% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Fatigue | grade 3-4, 1.1% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Rash | grade 3-4, 1.1% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Fatigue | grade 3-4, 1.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Mucosal inflammation | grade 3-4, 1.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Nausea | grade 3-4, 1.4% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Alanine aminotransferase increased | grade 3-4, 2.1% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Stomatitis | grade 3-4, 2.1% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Lipase increased | grade 3-4, 3.5% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Hyperglycaemia | grade 3-4, 31.3% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Hyperglycemia | grade 3-4, 4.2% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Diarrhoea | grade 3-4, 5.6% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Rash maculo-papular | grade 3-4, 8.8% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Rash | grade 3-4, 9.2% Disc. AE |
300 mg 1 times / day steady, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Co-administed with:: fulvestrant(500 mg was administered intramuscularly on Cycle 1, Day 1 and 15 and then at Day 1 of each 28-day cycle during treatment phase) Sources: Page: p. 138 |
unhealthy, 63 years (range: 25 - 92 years) n = 284 Health Status: unhealthy Age Group: 63 years (range: 25 - 92 years) Sex: M+F Population Size: 284 Sources: Page: p. 138 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
low [Ki 1.38 uM] | ||||
no [EC50 26 uM] | ||||
no [EC50 34 uM] | ||||
no [EC50 66 uM] | ||||
no [Ki 101.5 uM] | ||||
no [Ki 139.6 uM] | ||||
no [Ki 190.8 uM] | ||||
no [Ki 20.9 uM] | ||||
no [Ki 215.5 uM] | ||||
no [Ki 29.4 uM] | ||||
no [Ki 36 uM] | ||||
no [Ki 40 uM] | ||||
no [Ki 42.4 uM] | ||||
no [Ki 49.6 uM] | ||||
no [Ki 74.5 uM] | ||||
no [Ki 77.6 uM] | ||||
no [Ki 8.59 uM] | ||||
no [Ki 91.6 uM] | ||||
no [Ki >175 uM] | ||||
yes [EC50 2.2 uM] | ||||
yes [EC50 3 uM] | ||||
yes [Ki 96.7 uM] | ||||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [Km 2 uM] | ||||
yes [Km 24.95 uM] |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. | 2013 Jul 1 |
|
Absorption, distribution, metabolism, and excretion of [(14)C]BYL719 (alpelisib) in healthy male volunteers. | 2015 Oct |
|
PI3K inhibitors as new cancer therapeutics: implications for clinical trial design. | 2016 |
|
Activation of the PI3K/mTOR Pathway following PARP Inhibition in Small Cell Lung Cancer. | 2016 |
|
[Current Progress and Feasibility of Using Molecular-Targeted Agent Combinations for Metastatic Colorectal Cancer]. | 2016 Apr |
|
Treatment strategies for advanced hormone receptor-positive and human epidermal growth factor 2-negative breast cancer: the role of treatment order. | 2016 Jan |
|
PI3Kα inhibition reduces obesity in mice. | 2016 Nov 4 |
|
A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer. | 2017 Jan 1 |
Sample Use Guides
Alpelisib (300 mg once daily) in combination with fulvestrant (500 mg; intramuscular injection on day 1 and day 15 of cycle 1, and then day 1 of each subsequent 28-day cycle) for men and postmenopausal women with hormone receptor positive, HER2-negative advanced breast cancer which progressed on or after aromatase inhibitor treatment.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27126994
Overexpression of FGFR1 in ER+/PIK3CA mutant breast cancer cells attenuated the response to alpelisib in vitro .
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 06:49:18 GMT 2023
by
admin
on
Sat Dec 16 06:49:18 GMT 2023
|
Record UNII |
08W5N2C97Q
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
930022
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
||
|
FDA ORPHAN DRUG |
710819
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
||
|
NCI_THESAURUS |
C2152
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
||
|
NCI_THESAURUS |
C129825
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
EF-18
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
2169285
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
DB12015
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
100000166553
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
Alpelisib
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
56649450
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
5328
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
DTXSID70153355
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
m12147
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
C94214
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
9833
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
SUB180707
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
08W5N2C97Q
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
CHEMBL2396661
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
1217486-61-7
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY | |||
|
08W5N2C97Q
Created by
admin on Sat Dec 16 06:49:19 GMT 2023 , Edited by admin on Sat Dec 16 06:49:19 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TRANSPORTER -> INHIBITOR |
The in vitro study result indicated that alpelisib is a weak P-gp inhibitor with a Ki of 98.6 μM (R0900459).
Ki
|
||
|
TARGET -> INHIBITOR |
IC50
|
||
|
TARGET -> INHIBITOR |
IC50
|
||
|
TARGET -> INHIBITOR |
IC50
|
||
|
OFF-TARGET->INHIBITOR |
IC50
|
||
|
TARGET -> INHIBITOR |
IC50
|
||
|
OFF-TARGET->INHIBITOR |
IC50
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
||
|
BINDER->LIGAND |
In vitro, protein binding of alpelisib is 89% and is independent of concentration.
|
||
|
TRANSPORTER -> SUBSTRATE |
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
|
||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL
|
||
|
METABOLIC ENZYME -> INHIBITOR |
In vitro, alpelisib is a strong time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
Ki
|
||
|
METABOLIC ENZYME -> INDUCER |
STRONG
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
MAJOR
FECAL; PLASMA; URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Tmax | PHARMACOKINETIC |
|
|
|||
Biological Half-life | PHARMACOKINETIC |
|
|
|||
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
blood-to-plasma ratio | PHARMACOKINETIC |
|
|
|||