Table of Contents Table of Contents 2 List of Tables 6 List of Figures 6 Introduction 7 Global Markets Direct Report Coverage 7 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Overview 9 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Therapeutics Development 10 Products under Development by Stage of Development 10 Products under Development by Therapy Area 11 Products under Development by Indication 12 Products under Development by Companies 16 Products under Development by Universities/Institutes 22 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Therapeutics Assessment 24 Assessment by Mechanism of Action 24 Assessment by Route of Administration 25 Assessment by Molecule Type 26 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Companies Involved in Therapeutics Development 27 AstraZeneca Plc 27 Bayer AG 27 Curis Inc 28 Eli Lilly and Co 29 Genentech Inc 30 GlaxoSmithKline Plc 30 Millennium Pharmaceuticals Inc 31 Novartis AG 31 Onconova Therapeutics Inc 33 PIQUR Therapeutics AG 33 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Drug Profiles 35 alpelisib - Drug Profile 35 Product Description 35 Mechanism Of Action 35 R&D Progress 35 BAY-1082439 - Drug Profile 39 Product Description 39 Mechanism Of Action 39 R&D Progress 39 Bimiralisib - Drug Profile 40 Product Description 40 Mechanism Of Action 40 R&D Progress 40 buparlisib hydrochloride - Drug Profile 43 Product Description 43 Mechanism Of Action 43 R&D Progress 43 fimepinostat - Drug Profile 50 Product Description 50 Mechanism Of Action 50 R&D Progress 50 GDC-0077 - Drug Profile 56 Product Description 56 Mechanism Of Action 56 R&D Progress 56 LY-3023414 - Drug Profile 57 Product Description 57 Mechanism Of Action 57 R&D Progress 57 NSC-765844 - Drug Profile 60 Product Description 60 Mechanism Of Action 60 R&D Progress 60 omipalisib - Drug Profile 61 Product Description 61 Mechanism Of Action 61 R&D Progress 61 ON-146040 - Drug Profile 62 Product Description 62 Mechanism Of Action 62 R&D Progress 62 PQR-514 - Drug Profile 63 Product Description 63 Mechanism Of Action 63 R&D Progress 63 PQR-530 - Drug Profile 64 Product Description 64 Mechanism Of Action 64 R&D Progress 64 serabelisib - Drug Profile 65 Product Description 65 Mechanism Of Action 65 R&D Progress 65 SF-2523 - Drug Profile 67 Product Description 67 Mechanism Of Action 67 R&D Progress 67 Small Molecule to Inhibit PI3K Alpha for Cancer - Drug Profile 69 Product Description 69 Mechanism Of Action 69 R&D Progress 69 Small Molecules to Inhibit Pan PI3K for Ovarian Cancer - Drug Profile 70 Product Description 70 Mechanism Of Action 70 R&D Progress 70 Small Molecules to Inhibit PI3K Alpha for Breast Cancer - Drug Profile 71 Product Description 71 Mechanism Of Action 71 R&D Progress 71 SPR-965 - Drug Profile 72 Product Description 72 Mechanism Of Action 72 R&D Progress 72 taselisib - Drug Profile 73 Product Description 73 Mechanism Of Action 73 R&D Progress 73 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Dormant Products 77 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Discontinued Products 79 Phosphatidylinositol 4,5 Bisphosphate 3 Kinase Catalytic Subunit Alpha Isoform (Phosphatidylinositol 4,5 Bisphosphate 3 Kinase 110 kDa Catalytic Subunit Alpha or Phosphoinositide 3 Kinase Catalytic Alpha Polypeptide or Serine/Threonine Protein Kinase PIK3CA or PIK3CA or EC 2.7.11.1 or EC 2.7.1.153) - Product Development Milestones 81 Featured News & Press Releases 81 Sep 25, 2017: SignalRx Presents in silico Design of Dual PI3K/BRD4 Inhibitors for Combinatorial Activation of Anti-tumor Immunity in Treating Cancer 81 Sep 08, 2017: LORELEI: Taselisib Boosts Breast Tumor Shrinkage 81 May 25, 2017: Curis Announces Presentation Related to CUDC-907 at 2017 ASCO Annual Meeting 83 May 01, 2017: SignalRx Discloses its Novel Immuno-Oncology Program Approach at the 12th Annual Drug Discovery Chemistry 2017 Meeting 83 Apr 27, 2017: PIQUR Receives EMA Orphan Drug Designation for PQR309 in Diffuse Large B-Cell Lymphoma 84 Feb 01, 2017: SignalRx Pharmaceuticals Announces Breakthrough Results on Novel Anti-Cancer Dual PI3K-BRD4 Inhibition Paradigm in PNAS Publication 84 Dec 12, 2016: PI3K Inhibitor Buparlisib in Combination with Fulvestrant Prolongs PFS Compared to Placebo Plus Fulvestrant 85 Jun 08, 2016: Curis Announces Oral Presentation of Clinical Data Update from the Phase 1 Study of CUDC-907 at the 21st Congress of the European Hematology Association 86 Jun 02, 2016: Curis Announces Presentations Related to CUDC-907 at 2016 ASCO Annual Meeting 87 Apr 11, 2016: Curis Announces Presentation of Preclinical Data for CUDC-907 at AACR Annual Meeting 87 Apr 04, 2016: Curis Announces Publication of CUDC-907 Phase 1 Clinical Trial Data in Lancet Oncology 87 Jan 11, 2016: Seahorse Bioscience XF Technology Reaches 500th Citation in Cancer Research 88 Dec 06, 2015: Curis Reports Clinical Activity of CUDC-907 in Patients With DLBCL Harboring MYC Oncogene Alterations at the 2015 ASH Annual Meeting 89 Nov 05, 2015: Curis Announces Oral Presentation of Phase 1 Data for CUDC-907 at 2015 ASH Annual Meeting 90 Jun 17, 2015: Eli Lilly and Company Enters Into Strategic Partnership with Sarah Cannon Research Institute to Develop Investigational Oncology Therapy 91 Appendix 92 Methodology 92 Coverage 92 Secondary Research 92 Primary Research 92 Expert Panel Validation 92 Contact Us 92 Disclaimer 93

List of Tables Number of Products under Development by Stage of Development, H2 2017 10 Number of Products under Development by Therapy Areas, H2 2017 11 Number of Products under Development by Indications, H2 2017 12 Number of Products under Development by Indications, H2 2017 (Contd..1), H2 2017 14 Number of Products under Development by Indications, H2 2017 (Contd..2), H2 2017 15 Number of Products under Development by Companies, H2 2017 16 Products under Development by Companies, H2 2017 17 Products under Development by Companies, H2 2017 (Contd..1), H2 2017 18 Products under Development by Companies, H2 2017 (Contd..2), H2 2017 19 Products under Development by Companies, H2 2017 (Contd..3), H2 2017 20 Products under Development by Companies, H2 2017 (Contd..4), H2 2017 21 Number of Products under Investigation by Universities/Institutes, H2 2017 22 Products under Investigation by Universities/Institutes, H2 2017 23 Number of Products by Stage and Mechanism of Actions, H2 2017 24 Number of Products by Stage and Route of Administration, H2 2017 25 Number of Products by Stage and Molecule Type, H2 2017 26 Pipeline by AstraZeneca Plc, H2 2017 27 Pipeline by Bayer AG, H2 2017 28 Pipeline by Curis Inc, H2 2017 29 Pipeline by Eli Lilly and Co, H2 2017 30 Pipeline by Genentech Inc, H2 2017 30 Pipeline by GlaxoSmithKline Plc, H2 2017 31 Pipeline by Millennium Pharmaceuticals Inc, H2 2017 31 Pipeline by Novartis AG, H2 2017 32 Pipeline by Onconova Therapeutics Inc, H2 2017 33 Pipeline by PIQUR Therapeutics AG, H2 2017 34 Dormant Products, H2 2017 77 Dormant Products, H2 2017 (Contd..1), H2 2017 78 Discontinued Products, H2 2017 79 Discontinued Products, H2 2017 (Contd..1), H2 2017 80 List of Figures Number of Products under Development by Stage of Development, H2 2017 10 Number of Products under Development by Therapy Areas, H2 2017 11 Number of Products under Development by Top 10 Indications, H2 2017 12 Number of Products by Stage and Mechanism of Actions, H2 2017 24 Number of Products by Stage and Route of Administration, H2 2017 25 Number of Products by Stage and Molecule Type, H2 2017 26

AstraZeneca Plc Bayer AG Curis Inc Eli Lilly and Co Genentech Inc GlaxoSmithKline Plc Millennium Pharmaceuticals Inc Novartis AG Onconova Therapeutics Inc PIQUR Therapeutics AG