Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Bechter, Oliver
Dumez, Herlinde
Costermans, Jo
Punie, Kevin
Hsu, Karl
Dedieu, Jean-François
Ghuysen, Anne-Frédérique
Francesconi, Elisa
Sharma, Jyoti
Liu, Li
Schöffski, Patrick

Open PDF

Open link

Publication date

July 2016

DOI

10.1007/s00280-016-3056-0

Publisher

Springer-Verlag

ISSN

0344-5704

Journal

0344-5704

Abstract

Pilaralisib (SAR245408), a pan-class I PI3K inhibitor, has been investigated in Phase I/II trials in several solid tumors and lymphomas in capsule and tablet formulations of polymorph A (capsule-A and tablet-A). This Phase I study was conducted to determine the recommended Phase II dose (RP2D) of a more thermodynamically stable form of pilaralisib (polymorph E), in tablet formulation (tablet-E), in patients with advanced solid tumors or relapsed/refractory lymphoma.status: publishe

Extracted data

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Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Bechter, Oliver
Dumez, Herlinde
Costermans, Jo
Punie, Kevin
Hsu, Karl
Dedieu, Jean-François
Ghuysen, Anne-Frédérique
Francesconi, Elisa
Sharma, Jyoti
Liu, Li
Schöffski, Patrick

Open PDF

Open link

Publication date

July 2016

DOI

10.1007/s00280-016-3056-0

Publisher

Springer-Verlag

ISSN

0344-5704

Journal

0344-5704

Abstract

Extracted data

Soria, Jean-Charles
Adjei, Alex A.
Bahleda, Rastilav
Besse, Benjamin
Ferte, Charles
Planchard, David
Zhou, Jing
Ware, Joseph
Morrissey, Kari
Shankar, Geetha
Lin, Wei
Schutzman, Jennifer L.
Dy, Grace K.
Groen, Harry J. M.

November 2017

Aim: The phosphatidylinositol 3-kinase (PI3K) pathway is a potential therapeutic target in non-small...

Phase I Safety and Pharmacokinetic Study of the PI3K/mTOR Inhibitor SAR245409 (XL765) in Combination with Erlotinib in Patients with Advanced Solid Tumors

Jänne, Pasi A.
Cohen, Roger B.
Laird, A. Douglas
Macé, Sandrine
Engelman, Jeffrey A.
Ruiz-Soto, Rodrigo
Rockich, Kevin
Xu, Jianbo
Shapiro, Geoffrey I.
Martinez, Pablo
Felip, Enriqueta

March 2014

Introduction:The primary objectives of this phase I study were to evaluate the safety and maximum to...

A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies.

Juric, D
de Bono, JS
LoRusso, PM
Nemunaitis, J
Heath, EI
Kwak, EL
Macarulla Mercadé, T
Geuna, E
Jose de Miguel-Luken, M
Patel, C
Kuida, K
Sankoh, S
Westin, EH
Zohren, F
Shou, Y
Tabernero, J

September 2017

Purpose: To evaluate the safety, MTD, pharmacokinetics, pharmacodynamics, and preliminary antitumor ...

Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Bechter, Oliver
Dumez, Herlinde
Costermans, Jo
Punie, Kevin
Hsu, Karl
Dedieu, Jean-François
Ghuysen, Anne-Frédérique
Francesconi, Elisa
Sharma, Jyoti
Liu, Li
Schöffski, Patrick

July 2016

Pilaralisib (SAR245408), a pan-class I PI3K inhibitor, has been investigated in Phase I/II trials in...

Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan‐Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

Edelman, Gerald
Rodon, Jordi
Lager, Joanne
Castell, Christelle
Jiang, Jason
Van Allen, Eliezer M.
Wagle, Nikhil
Lindeman, Neal I.
Sholl, Lynette M.
Shapiro, Geoffrey I.

May 2018

Abstract Lessons Learned. A phase I study of the pan‐class I phosphoinositide 3‐kinase inhibitor pil...

Phosphatidylinositol 3-Kinase -Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

Juric, Dejan
Rodon, Jordi
Tabernero Caturla, Josep
Janku, Filip
Burris, Howard A.
Schellens, Jan H. M.
Middleton, Mark R.
Berlin, Jordan
Schuler, Martin
Gil-Martín, Marta
Rugo, Hope S.
Seggewiss Bernhardt, Ruth
Huang, Alan
Bootle, Douglas
Demanse, David
Blumenstein, Lars
Coughlin, Christina
Quadt, Cornelia
Baselga Torres, Josep, 1959-

December 2020

PurposeWe report the first-in-human phase Ia study to our knowledge (ClinicalTrials.gov identifier: ...

First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.

Sarker, Debashis
Ang, Joo Ern
Baird, Richard
Kristeleit, Rebecca
Shah, Krunal
Moreno, Victor
Clarke, Paul A
Raynaud, Florence I
Levy, Gallia
Ware, Joseph A
Mazina, Kathryn
Lin, Ray
Wu, Jenny
Fredrickson, Jill
Spoerke, Jill M
Lackner, Mark R
Yan, Yibing
Friedman, Lori S
Kaye, Stan B
Derynck, Mika K
Workman, Paul
de Bono, Johann S

January 2015

PURPOSE: This first-in-human dose-escalation trial evaluated the safety, tolerability, maximal-toler...

First-in-Human Phase I Study of Pictilisib (GDC-0941), a Potent Pan-Class I Phosphatidylinositol-3-Kinase (PI3K) Inhibitor, in Patients with Advanced Solid Tumors

Sarker, Debashis
Ang, Joo Ern
Baird, Richard
Kristeleit, Rebecca
Shah, Krunal
Moreno, Victor
Clarke, Paul A
Raynaud, Florence I
Levy, Gallia
Ware, Joseph A
Mazina, Kathryn
Lin, Ray
Wu, Jenny
Fredrickson, Jill
Spoerke, Jill M
Lackner, Mark R
Yan, Yibing
Friedman, Lori S
Kaye, Stan B
Derynck, Mika K
Workman, Paul
de Bono, Johann S

January 2015

PURPOSE: This first-in-human dose-escalation trial evaluated the safety, tolerability, maximal-toler...

A Multi-Arm Phase I Study of the PI3K/mTOR Inhibitors PF-04691502 and Gedatolisib (PF-05212384) plus Irinotecan or the MEK Inhibitor PD-0325901 in Advanced Cancer

Wainberg, Zev A.
Alsina Maqueda, Maria
Soares, Heloisa P.
Braña, Irene
Britten, Carolyn D.
Del Conte, Gianluca
Ezeh, Patrick
Houk, Brett
Kern, Kenneth A.
Leong, Stephen
Pathan, Nuzhat
Pierce, Kristen J.
Siu, Lillian L.
Vermette, Jennifer
Tabernero, Josep
Universitat Autònoma de Barcelona

January 2017

Ajuts: This study was sponsored by Pfizer Inc.This phase I, four-arm, open-label study (NCT01347866)...

First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer

Blagden S.
Olmin A.
Josephs D.
Stavraka C.
Zivi A.
Pinato D. J.
Anthoney A.
Decordova S.
Swales K.
Riisnaes R.
Pope L.
Noguchi K.
Shiokawa R.
Inatani M.
Prince J.
Jones K.
Twelves C.
Spicer J.
Banerji U.

January 2014

Purpose: This phase I dose-escalation study investigated the maximum-tolerated dose (MTD), dose-limi...

First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies

Munster, Pamela
Aggarwal, Rahul
Hong, David
Schellens, Jan H.M.
Van Der Noll, Ruud
Specht, Jennifer
Witteveen, Petronella O.
Werner, Theresa L.
Dees, E. Claire
Bergsland, Emily
Agarwal, Neeraj
Kleha, Joseph F.
Durante, Michael
Adams, Laurel
Smith, Deborah A.
Lampkin, Thomas A.
Morris, Shannon R.
Kurzrock, Razelle

January 2016

GSK2126458 (GSK458) is a potent inhibitor of PI3K (α, β, γ, and δ), with preclinical studies demonst...

Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma

Dreyling, Martin
Vitolo, Umberto
Hiemeyer, Florian
Giurescu, Marius
Garcia-Vargas, José
Gorbatchevsky, Igor
Liu, Li
Koechert, Karl
Peña, Carol
Neves, M.
Childs, Barrett B.H.
Morschhauser, Franck
Zinzani, Piér P.L.
Bouabdallah, Krimo
Bron, Dominique
Cunningham, David
Assouline, Sarit S.E.
Verhoef, Gregor E G
Linton, Kim
Thieblemont, Catherine

January 2017

Background: Copanlisib is a pan-class I phosphatidylinositol 3-kinase inhibitor with predominant act...

A phase I study investigating AZD8186, a potent and selective inhibitor of PI3Kβ/δ, in patients with advanced solid tumors.

Choudhury, AD
Higano, CS
de Bono, JS
Cook, N
Rathkopf, DE
Wisinski, KB
Martin-Liberal, J
Linch, M
Heath, EI
Baird, RD
Garcia-Corbacho, J
Quintela-Fandino, M
Barry, ST
de Bruin, EC
Colebrook, S
Hawkins, G
Klinowska, T
Maroj, B
Moorthy, G
Mortimer, PG
Moschetta, M
Nikolaou, M
Sainsbury, L
Shapiro, GI
Siu, LL
Hansen, AR

March 2022

To characterize safety and tolerability of the selective PI3Kβ inhibitor AZD8186, identify a recomme...

Soria, Jean-Charles
Adjei, Alex A.
Bahleda, Rastilav
Besse, Benjamin
Ferte, Charles
Planchard, David
Zhou, Jing
Ware, Joseph
Morrissey, Kari
Shankar, Geetha
Lin, Wei
Schutzman, Jennifer L.
Dy, Grace K.
Groen, Harry J. M.

November 2017

Aim: The phosphatidylinositol 3-kinase (PI3K) pathway is a potential therapeutic target in non-small...

Phase I Safety and Pharmacokinetic Study of the PI3K/mTOR Inhibitor SAR245409 (XL765) in Combination with Erlotinib in Patients with Advanced Solid Tumors

Jänne, Pasi A.
Cohen, Roger B.
Laird, A. Douglas
Macé, Sandrine
Engelman, Jeffrey A.
Ruiz-Soto, Rodrigo
Rockich, Kevin
Xu, Jianbo
Shapiro, Geoffrey I.
Martinez, Pablo
Felip, Enriqueta

March 2014

Introduction:The primary objectives of this phase I study were to evaluate the safety and maximum to...

A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies.

Juric, D
de Bono, JS
LoRusso, PM
Nemunaitis, J
Heath, EI
Kwak, EL
Macarulla Mercadé, T
Geuna, E
Jose de Miguel-Luken, M
Patel, C
Kuida, K
Sankoh, S
Westin, EH
Zohren, F
Shou, Y
Tabernero, J

September 2017

Purpose: To evaluate the safety, MTD, pharmacokinetics, pharmacodynamics, and preliminary antitumor ...

Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Bechter, Oliver
Dumez, Herlinde
Costermans, Jo
Punie, Kevin
Hsu, Karl
Dedieu, Jean-François
Ghuysen, Anne-Frédérique
Francesconi, Elisa
Sharma, Jyoti
Liu, Li
Schöffski, Patrick

July 2016

Pilaralisib (SAR245408), a pan-class I PI3K inhibitor, has been investigated in Phase I/II trials in...

Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan‐Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

Edelman, Gerald
Rodon, Jordi
Lager, Joanne
Castell, Christelle
Jiang, Jason
Van Allen, Eliezer M.
Wagle, Nikhil
Lindeman, Neal I.
Sholl, Lynette M.
Shapiro, Geoffrey I.

May 2018

Abstract Lessons Learned. A phase I study of the pan‐class I phosphoinositide 3‐kinase inhibitor pil...

Phosphatidylinositol 3-Kinase -Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

Juric, Dejan
Rodon, Jordi
Tabernero Caturla, Josep
Janku, Filip
Burris, Howard A.
Schellens, Jan H. M.
Middleton, Mark R.
Berlin, Jordan
Schuler, Martin
Gil-Martín, Marta
Rugo, Hope S.
Seggewiss Bernhardt, Ruth
Huang, Alan
Bootle, Douglas
Demanse, David
Blumenstein, Lars
Coughlin, Christina
Quadt, Cornelia
Baselga Torres, Josep, 1959-

December 2020

PurposeWe report the first-in-human phase Ia study to our knowledge (ClinicalTrials.gov identifier: ...

First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.

Sarker, Debashis
Ang, Joo Ern
Baird, Richard
Kristeleit, Rebecca
Shah, Krunal
Moreno, Victor
Clarke, Paul A
Raynaud, Florence I
Levy, Gallia
Ware, Joseph A
Mazina, Kathryn
Lin, Ray
Wu, Jenny
Fredrickson, Jill
Spoerke, Jill M
Lackner, Mark R
Yan, Yibing
Friedman, Lori S
Kaye, Stan B
Derynck, Mika K
Workman, Paul
de Bono, Johann S

January 2015

PURPOSE: This first-in-human dose-escalation trial evaluated the safety, tolerability, maximal-toler...

First-in-Human Phase I Study of Pictilisib (GDC-0941), a Potent Pan-Class I Phosphatidylinositol-3-Kinase (PI3K) Inhibitor, in Patients with Advanced Solid Tumors

Sarker, Debashis
Ang, Joo Ern
Baird, Richard
Kristeleit, Rebecca
Shah, Krunal
Moreno, Victor
Clarke, Paul A
Raynaud, Florence I
Levy, Gallia
Ware, Joseph A
Mazina, Kathryn
Lin, Ray
Wu, Jenny
Fredrickson, Jill
Spoerke, Jill M
Lackner, Mark R
Yan, Yibing
Friedman, Lori S
Kaye, Stan B
Derynck, Mika K
Workman, Paul
de Bono, Johann S

January 2015

PURPOSE: This first-in-human dose-escalation trial evaluated the safety, tolerability, maximal-toler...

A Multi-Arm Phase I Study of the PI3K/mTOR Inhibitors PF-04691502 and Gedatolisib (PF-05212384) plus Irinotecan or the MEK Inhibitor PD-0325901 in Advanced Cancer

Wainberg, Zev A.
Alsina Maqueda, Maria
Soares, Heloisa P.
Braña, Irene
Britten, Carolyn D.
Del Conte, Gianluca
Ezeh, Patrick
Houk, Brett
Kern, Kenneth A.
Leong, Stephen
Pathan, Nuzhat
Pierce, Kristen J.
Siu, Lillian L.
Vermette, Jennifer
Tabernero, Josep
Universitat Autònoma de Barcelona

January 2017

Ajuts: This study was sponsored by Pfizer Inc.This phase I, four-arm, open-label study (NCT01347866)...

First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer

Blagden S.
Olmin A.
Josephs D.
Stavraka C.
Zivi A.
Pinato D. J.
Anthoney A.
Decordova S.
Swales K.
Riisnaes R.
Pope L.
Noguchi K.
Shiokawa R.
Inatani M.
Prince J.
Jones K.
Twelves C.
Spicer J.
Banerji U.

January 2014

Purpose: This phase I dose-escalation study investigated the maximum-tolerated dose (MTD), dose-limi...

First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies

Munster, Pamela
Aggarwal, Rahul
Hong, David
Schellens, Jan H.M.
Van Der Noll, Ruud
Specht, Jennifer
Witteveen, Petronella O.
Werner, Theresa L.
Dees, E. Claire
Bergsland, Emily
Agarwal, Neeraj
Kleha, Joseph F.
Durante, Michael
Adams, Laurel
Smith, Deborah A.
Lampkin, Thomas A.
Morris, Shannon R.
Kurzrock, Razelle

January 2016

GSK2126458 (GSK458) is a potent inhibitor of PI3K (α, β, γ, and δ), with preclinical studies demonst...

Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma

Dreyling, Martin
Vitolo, Umberto
Hiemeyer, Florian
Giurescu, Marius
Garcia-Vargas, José
Gorbatchevsky, Igor
Liu, Li
Koechert, Karl
Peña, Carol
Neves, M.
Childs, Barrett B.H.
Morschhauser, Franck
Zinzani, Piér P.L.
Bouabdallah, Krimo
Bron, Dominique
Cunningham, David
Assouline, Sarit S.E.
Verhoef, Gregor E G
Linton, Kim
Thieblemont, Catherine

January 2017

Background: Copanlisib is a pan-class I phosphatidylinositol 3-kinase inhibitor with predominant act...

A phase I study investigating AZD8186, a potent and selective inhibitor of PI3Kβ/δ, in patients with advanced solid tumors.

Choudhury, AD
Higano, CS
de Bono, JS
Cook, N
Rathkopf, DE
Wisinski, KB
Martin-Liberal, J
Linch, M
Heath, EI
Baird, RD
Garcia-Corbacho, J
Quintela-Fandino, M
Barry, ST
de Bruin, EC
Colebrook, S
Hawkins, G
Klinowska, T
Maroj, B
Moorthy, G
Mortimer, PG
Moschetta, M
Nikolaou, M
Sainsbury, L
Shapiro, GI
Siu, LL
Hansen, AR

March 2022

To characterize safety and tolerability of the selective PI3Kβ inhibitor AZD8186, identify a recomme...

Soria, Jean-Charles
Adjei, Alex A.
Bahleda, Rastilav
Besse, Benjamin
Ferte, Charles
Planchard, David
Zhou, Jing
Ware, Joseph
Morrissey, Kari
Shankar, Geetha
Lin, Wei
Schutzman, Jennifer L.
Dy, Grace K.
Groen, Harry J. M.

November 2017

Aim: The phosphatidylinositol 3-kinase (PI3K) pathway is a potential therapeutic target in non-small...

Phase I Safety and Pharmacokinetic Study of the PI3K/mTOR Inhibitor SAR245409 (XL765) in Combination with Erlotinib in Patients with Advanced Solid Tumors

Jänne, Pasi A.
Cohen, Roger B.
Laird, A. Douglas
Macé, Sandrine
Engelman, Jeffrey A.
Ruiz-Soto, Rodrigo
Rockich, Kevin
Xu, Jianbo
Shapiro, Geoffrey I.
Martinez, Pablo
Felip, Enriqueta

March 2014

Introduction:The primary objectives of this phase I study were to evaluate the safety and maximum to...

A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies.

Juric, D
de Bono, JS
LoRusso, PM
Nemunaitis, J
Heath, EI
Kwak, EL
Macarulla Mercadé, T
Geuna, E
Jose de Miguel-Luken, M
Patel, C
Kuida, K
Sankoh, S
Westin, EH
Zohren, F
Shou, Y
Tabernero, J

September 2017

Purpose: To evaluate the safety, MTD, pharmacokinetics, pharmacodynamics, and preliminary antitumor ...

Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Abstract

Extracted data

Phase I safety and pharmacokinetic dose-escalation study of pilaralisib polymorph E, a phosphoinositide 3-kinase inhibitor in tablet formulation, in patients with solid tumors or lymphoma

Abstract

Extracted data

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