Genentech: Tim Heffron | Director, Principal Scientist, Discovery Chemistry

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Scientists / Our Scientists

"Each day we work to extend and improve lives."

16

Years at Genentech

34

Publications

I joined the Discovery Chemistry department at Genentech as a Medicinal Chemist in 2005 after completing my PhD in organic chemistry at MIT. I now lead interdisciplinary teams focused on the discovery of new drugs to extend and improve people’s lives.

Featured Publication

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

ACS Med Chem Lett. 2016 Feb 16;7(4):351-6.

Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG.

As a chemist, my work can focus on designing drugs directed to whatever target is most compelling from a biological point of view without being confined to a particular therapeutic area. In my time at Genentech I have contributed to programs directed toward the discovery of new therapeutics for oncology (including cancer immunotherapy), neuro-oncology, neurology, and ophthalmology indications. Each program brings unique scientific challenges and a need to innovate to discover new medicines.

Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

Drug Metabolism and Disposition, ISSN: 1521009X

Xingrong Liu; Xiaorong Liang; Jenninfer LeCouter; Savita Ubhayakar; Jacob Chen; Jay Cheng; Tom Lee; Joe Lubach; Jim Nonomiya; Sheerin Latham; Cristine Quiason-Huynh; Eric G. Solon; Matthew Wright; Marcel Hop; Tim Heffron

Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer

Structure,

Ping Wu; Christopher J. Sneeringer; Keith E. Pitts; Eric S. Day; Bryan Chan; Binqing Wei; Isabelle Lehoux; Kyle Mortara; Hong Li; Jiansheng Wu; Yvonne Franke; John Moffat; Jane Grogan; Tim Heffron; Weiru Wang

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Sarah M. Bronner; Karl A. Merrick; Jeremy Murray; Laurent Salphati; John Moffat; Jodie Pang; Christopher Sneeringer; Nick Dompe; Patrick Cyr; Hans Purkey; Gladys de Leon Boenig; Jun Li; Aleksandr Kolesnikov; Larouche-Gauthier; Kwong Wah Lai; Xiaoli Shen; Samuel Aubert-Nicol; Yi-Chen Chen; Jonathan Cheong; James Crawford; Marc Hafner; Pouyan Haghshenas; Araz Jakalian; Jean-Philippe Leclerc; Ngiap-Kie Lim; Thomas O'Brien; Emile Plise; Shalan; Claudio Sturino; John Wai; Yang Xiao; Peter Yin; Zhao; Stephen Gould; Alan Olivero; Tim Heffron

From Discovery to Market Readiness: The Research and Development of the β-Sparing Phosphatidylinositol 3-Kinase Inhibitor Taselisib

ACS Symposium Series, ISSN: 19475918 00976156

Remy Angelaud; Steven Staben; Tim Heffron; Andreas M. Schuster; Frederic St-Jean

Challenges of developing small-molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels

Neuro-Oncology, ISSN: 15235866 15228517

Tim Heffron

Brain distribution and efficacy of the brain penetrant PI3K inhibitor GDC-0084 in orthotopic mouse models of human glioblastoma

Drug Metabolism and Disposition, ISSN: 1521009X

Laurent Salphati; Bruno Alicke; Tim Heffron; Sheerin Latham; Merry Nishimura; Cao; Rick Carano; Jonathan Cheong; Joan Greve; Hartmut Koeppen; Shari Lau; Leslie Lee; Michelle Nannini; Jodie Pang; Emile Plise; Cristine Quiason; Linda Rangell; Xiaolin Zhang; Stephen Gould; Heidi Phillips; Alan Olivero

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Journal of Medicinal Chemistry, ISSN: 15204804

Bryan Chan; Emily Hanan; Krista Bowman; Callie Bryan; Dan Burdick; Emily Chan; Yuan Chen; Saundra Clausen; Trisha Dela Vega; Jenna Dotson; Charles Eigenbrot; Richard Elliott; Robert Heald; Philip Jackson; Jamie D. Knight; Hank La; Michael Lainchbury; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen M. Seward; Steve Sideris; Lily Shao; Shumei Wang; Siew Kuen Yeap; Ivana Yen; Christine Yu; Tim Heffron

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

ACS Medicinal Chemistry Letters, ISSN: 19485875

Tim Heffron; Chudi Ndubaku; Laurent Salphati; Bruno Alicke; Jonathan Cheong; Joy Drobnick; Kyle Edgar; Stephen Gould; Leslie Lee; John Lesnick; Cris Lewis; Jim Nonomiya; Jodie Pang; Emile Plise; Steve Sideris; Jeffrey Wallin; Lan Wang; Xiaolin Zhang; Alan Olivero

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Journal of Medicinal Chemistry, ISSN: 15204804

Tim Heffron; Robert Heald; Chudi Ndubaku; Binqing Wei; Martin Augistin; Steven Do; Kyle Edgar; Charles Eigenbrot; Lori Friedman; Emanuela Gancia; Philip Jackson; Graham Jones; Aleksandr Kolesnikov; Leslie B. Lee; John Lesnick; Cris Lewis; Neville J. McLean; Mario Mörtl; Jim Nonomiya; Jodie Pang; Steve Price; Wei Wei Prior; Laurent Salphati; Steve Sideris; Steven Staben; Stefan Steinbacher; Vickie Tsui; Jeffrey Wallin; Deepak Sampath; Alan Olivero

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 14643405

Emily Hanan; Matt Baumgardner; Callie Bryan; Yuan Chen; Charles Eigenbrot; Peter Fan; Xiao-Hui Gu; Hank La; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Steve Sideris; Ivana Yen; Christine Yu; Tim Heffron

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR

ACS Medicinal Chemistry Letters, ISSN: 19485875

Callie Bryan; Dan Burdick; Bryan Chan; Yuan Chen; Saundra Clausen; Jenna Dotson; Charles Eigenbrot; Richard Elliott; Emily Hanan; Robert Heald; Philip Jackson; Hank La; Michael Lainchbury; Shiva Malek; Sam E. Mann; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen Seward; Steve Sideris; Shumei Wang; Ivana Yen; Christine Yu; Tim Heffron

The Discovery and Process Chemistry Development of GDC-0084, a Brain Penetrating Inhibitor of PI3K and mTOR

ACS Symposium Series, ISSN: 19475918

Tim Heffron; Andrew McClory; Andy Stumpf

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Journal of Medicinal Chemistry, ISSN: 15204804

Robert Heald; Krista Bowman; Callie Bryan; Dan Burdick; Bryan Chan; Emily Chan; Yuan Chen; Saundra Clausen; Belen Dominguez-Fernandez; Charles Eigenbrot; Richard Elliott; Emily Hanan; Philip Jackson; Jamie Knight; Hank La; Michael Lainchbury; Shiva Malek; Sam E. Mann; Mark Merchant; Kyle Mortara; Hans Purkey; Gabriele Schaefer; Stephen Schmidt; Eileen Seward; Steve Sideris; Lily Shao; Shumei Wang; Kuen Yeap; Ivana Yen; Christine Yu; Tim Heffron

A probabilistic method to report predictions from a human liver microsomes stability QSAR model: A practical tool for drug discovery

Journal of Computer-Aided Molecular Design, ISSN: 15734951

Ignacio Aliagas; Alberto Gobbi; Tim Heffron; Man Ling Lee; Dan Ortwine; Mark Zak; Cyrus Khojasteh

CNS Anticancer Drug Discovery and Development Conference White Paper

Neuro-Oncology, ISSN: 15235866

Victor A. Levin; Peter J. Tonge; James M. Gallo; Marc R. Birtwistle; Arvin C. Dar; Antonio Iavarone; Patrick J. Paddison; Tim Heffron; William F. Elmquist; Jean E. Lachowicz; Ted W. Johnson; Forest M. White; Joohee Sul; Smith; Wang Shen; Jann N. Sarkaria; Ramakrishna Samala; Patrick Y. Wen; Donald A. Berry; Russell C. Petter

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Journal of Medicinal Chemistry, ISSN: 15204804

Emily Hanan; Charles Eigenbrot; Callie Bryan; Dan Burdick; Bryan Chan; Yuan Chen; Jenna Dotson; Robert Heald; Philip Jackson; Hank La; Michael Lainchbury; Shiva Malek; Hans Purkey; Gabriele Schaefer; Steve Schmidt; Eileen M. Seward; Steve Sideris; Christine Tam; Shumei Wang; Siew Kuen Yeap; Ivana Yen; Peter Yin; Christine Yu; Inna Zilberleyb; Tim Heffron

Discovery of highly potent, selective, and brain-penetrant aminopyrazole Leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

Journal of Medicinal Chemistry, ISSN: 15204804

Tony Estrada; Bryan Chan; Charles Baker-Glenn; Alan Beresford; Dan Burdick; Mark Chambers; Huifen Chen; Sara Dominguez; Jenna Dotson; Jake Drummond; Mike Flagella; Reina Fuji; Andrew Gill; Jason Halladay; Seth Harris; Tim Heffron; Tracy Kleinheinz; Donna Lee; Claire Le Pichon; Xingrong Liu; Joe Lyssikatos; Andrew D. Medhurst; John Moffat; Kevin Nash; Kimberly Scearce-Levie; Zejuan Sheng; Daniel Shore; Susan Wong; Shuo Zhang; Xiaolin Zhang; Haitao Zhu; Zach Sweeney

Prevalence of acid-reducing agents (ARA) in cancer populations and ARA drug-drug interaction potential for molecular targeted agents in clinical development

Molecular Pharmaceutics, ISSN: 15438384

Gillian S. Smelick; Tim Heffron; Laura Chu; Brian Dean; David West; Scott L. Duvall; Bert Lum; Nageshwar Budha; Scott Holden; Leslie Z. Benet; Adam Frymoyer; Mark Dresser; Joseph Ware

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d ][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2- methylpropanamide (GDC-0032): A β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity

Journal of Medicinal Chemistry, ISSN: 00222623

Chudi Ndubaku; Tim Heffron; Steven Staben; Matt Baumgardner; Nicole Blaquiere; Erin Bradley; Richard J. Bull; Steven Do; Jenna Dotson; Danette Dudley; Kyle Edgar; Lori Friedman; Rich Goldsmith; Robert Heald; Aleksandr Kolesnikov; Leslie Lee; Cris Lewis; Michelle Nannini; Jim Nonomiya; Jodie Pang; Steve Price; Wei Wei Prior; Laurent Salphati; Steve Sideris; Jeffrey Wallin; Lan Wang; Binqing Wei; Deepak Sampath; Alan Olivero

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Chudi Ndubaku; Nicole Blaquiere; Marcia Belvin; Richard J. Bull; Danette Dudley; Kyle Edgar; Daniel Gray; Robert Heald; Tim Heffron; Graham E. Jones; Mark Jones; Aleksandr Kolesnikov; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Neville J. McLean; Jim Nonomiya; Alan Olivero; Rachel Ord; Jodie Pang; Stephen Price; Wei Wei Prior; Lionel Rouge; Laurent Salphati; Deepak Sampath; Jeffrey Wallin; Lan Wang; Binqing Wei; Christian Weismann; Ping Wu

Noncovalent wild-type-sparing inhibitors of EGFR T790M

Cancer Discovery, ISSN: 21598274

Ho-June Lee; Gabriele Schaefer; Tim Heffron; Lily Shao; Xiaofen Ye; Steve Sideris; Shiva Malek; Emily Chan; Mark Merchant; Hank La; Savita Ubhayakar; Bob Yauch; Valentina Pirazzoli; Katerina Politi; Jeffrey Settleman

Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Nicole Blaquiere; Vickie Tsui; Aleksandr Kolesnikov; Steven Do; Erin Bradley; Jenna Dotson; Rich Goldsmith; Tim Heffron; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Alan Olivero; Jodie Pang; Lionel Rouge; Laurent Salphati; Binqing Wei; Christian Wiesmann; Ping Wu

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

Journal of Medicinal Chemistry, ISSN: 00222623

Tony Estrada; Xingrong Liu; Charles Baker-Glenn; Alan Beresford; Dan Burdick; Mark Chambers; Bryan Chan; Huifen Chen; Xiao Ding; Antonio DiPasquale; Sara Dominguez; Jenna Dotson; Jake Drummond; Mike Flagella; Sean Flynn; Reina Fuji; Andrew Gill; Janet Gunzner-Toste; Seth Harris; Tim Heffron; Tracy Kleinheinz; Donna Lee; Claire Le Pichon; Joe Lyssikatos; Andrew D. Medhurst; John Moffat; Susmith Mukund; Kevin Nash; Kimberly Scearce-Levie; Zejuan Sheng; Daniel Shore; Thuy Tran; Naimisha Trivedi; Shumei Wang; Shuo Zhang; Xiaolin Zhang; Guiling Zhao; Haitao Zhu; Zach Sweeney

Targeting the PI3K pathway in the brain - Efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

Clinical Cancer Research, ISSN: 10780432

Laurent Salphati; Tim Heffron; Bruno Alicke; Merry Nishimura; Kai Barck; Rick Carano; Jonathan Cheong; Kyle Edgar; Joan Greve; Samir Kharbanda; Hartmut Koeppen; Shari Lau; Leslie Lee; Jodie Pang; Emile Plise; Jenny L. Pokorny; Hani Bou-Reslan; Jann N. Sarkaria; Jeffrey Wallin; Xiaolin Zhang; Stephen Gould; Alan Olivero; Heidi Phillips

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α

Journal of Medicinal Chemistry, ISSN: 00222623

Tim Heffron; Laurent Salphati; Bruno Alicke; Jonathan Cheong; Jenna Dotson; Kyle Edgar; Rich Goldsmith; Stephen Gould; Leslie Lee; John Lesnick; Cris Lewis; Chudi Ndubaku; Jim Nonomiya; Alan Olivero; Jodie Pang; Emile Plise; Steve Sideris; Sean Trapp; Jeffrey Wallin; Lan Wang; Xiaolin Zhang

DEGAS: Sharing and tracking target compound ideas with external collaborators

Journal of Chemical Information and Modeling, ISSN: 15205142

Man Ling Lee; Ignacio Aliagas; Jenna Dotson; JW Feng; Alberto Gobbi; Tim Heffron

Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform

Journal of Medicinal Chemistry, ISSN: 00222623

Tim Heffron; Binqing Wei; Alan Olivero; Steven Staben; Vickie Tsui; Steven Do; Jenna Dotson; Adrian J. Folkes; Paul Goldsmith; Rich Goldsmith; Janet Gunzner-Toste; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Stephen Shuttleworth; Dan Sutherlin; Nan Chi Wan; Shumei Wang; Christian Wiesmann; Bing-Yan Zhu

Discovery of a potent, selective, and orally available class i phosphatidylinositol 3-kinase (PI3K)/Mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer

Journal of Medicinal Chemistry, ISSN: 00222623

Dan Sutherlin; Linda Bao; Megan Berry Swadell; Georgette Castanedo; Irina Chuckowree; Jenna Dotson; Adrian Folks; Lori Friedman; Rich Goldsmith; Janet Gunzner-Toste; Tim Heffron; John Lesnick; Cris Lewis; Simon Mathieu; Jeremy Murray; Jim Nonomiya; Jodie Pang; Neil Pegg; Wei Wei Prior; Lionel Rouge; Laurent Salphati; Deepak Sampath; Qingping Tian; Vickie Tsui; Nan Chi Wan; Shumei Wang; Binqing Wei; Christian Wiesmann; Ping Wu; Bing-Yan Zhu; Alan Olivero

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Mike Siu; Rich Goldsmith; Alan Olivero; Steven Do; Dan Burdick; Tim Heffron; Jenna Dotson; Dan Sutherlin; Bing-Yan Zhu; Vickie Tsui; Hoa Le; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Jodie Pang; Wei Wei Prior; Laurent Salphati; Lionel Rouge; Deepak Sampath; Steve Sideris; Christian Wiesmann; Ping Wu

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Steven Staben; Tim Heffron; Dan Sutherlin; Seema Bhat; Georgette Castanedo; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Lori Friedman; Leslie Lee; John Lesnick; Cris Lewis; Jeremy Murray; Jim Nonomiya; Alan Olivero; Emile Plise; Jodie Pang; Wei Wei Prior; Laurent Salphati; Lionel Rouge; Deepak Sampath; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Weismann; Ping Wu; Bing-Yan Zhu

Ladder polyether synthesis via epoxide-opening cascades directed by a disappearing trimethylsilyl group

Journal of Organic Chemistry, ISSN: 00223263

Tim Heffron; Graham L. Simpson; Estibaliz Merino; Timothy F. Jamison

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Bioorganic and Medicinal Chemistry Letters, ISSN: 0960894X

Tim Heffron; Megan Berry Swadell; Georgette Castanedo; Christine Chang; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Janet Gunzner-Toste; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; David Peterson; Laurent Salphati; Deepak Sampath; Steve Sideris; Dan Sutherlin; Vickie Tsui; Nan Chi Wan; Shumei Wang; Susan Wong; Bing-Yan Zhu

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available Pan-PI3-kinase and dual Pan-PI3-kinase/mTOR inhibitors for the treatment of cancer

Journal of Medicinal Chemistry, ISSN: 00222623

Dan Sutherlin; Deepak Sampath; Megan Berry Swadell; Georgette Castanedo; Zhigang Chang; Irina Chuckowree; Jenna Dotson; Adrian J. Folkes; Lori Friedman; Rich Goldsmith; Tim Heffron; Leslie Lee; John Lesnick; Cris Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; Wei Wei Prior; Laurent Salphati; Steve Sideris; Qingping Tian; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Wiesmann; Susan Wong; Bing-Yan Zhu

Concerning Lewis acid promoted, directing-group-free epoxide-ring-opening cascades

Synlett, ISSN: 09365214

Tim Heffron; Timothy F. Jamison

Massachusetts Institute of Technology, Organic Chemistry, Ph. D. – 2005
Yale University, Chemistry, B.S. – 2000