Table of Contents Table of Contents 2 List of Tables 6 List of Figures 7 Introduction 8 Global Markets Direct Report Coverage 8 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 Therapeutics Development 10 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) - Products under Development by Stage of Development 10 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) - Products under Development by Therapy Area 11 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) - Products under Development by Indication 12 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) - Pipeline Products Glance 15 Late Stage Products 15 Early Stage Products 16 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) - Products under Development by Companies 17 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) - Products under Development by Universities/Institutes 23 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 25 Assessment by Monotherapy/Combination Products 25 Assessment by Mechanism of Action 26 Assessment by Route of Administration 27 Assessment by Molecule Type 28 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 29 Bayer AG 29 Curis, Inc. 30 Eli Lilly and Company 31 Genentech, Inc. 32 GlaxoSmithKline Plc 33 Hutchison MediPharma Limited 34 Millennium Pharmaceuticals Inc 35 Novartis AG 36 PIQUR Therapeutics AG 38 Sphaera Pharma Pvt. Ltd. 39 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 40 alpelisib - Drug Profile 40 Product Description 40 Mechanism Of Action 40 R&D Progress 40 BAY-1082439 - Drug Profile 43 Product Description 43 Mechanism Of Action 43 R&D Progress 43 buparlisib hydrochloride - Drug Profile 44 Product Description 44 Mechanism Of Action 44 R&D Progress 44 CUDC-907 - Drug Profile 49 Product Description 49 Mechanism Of Action 49 R&D Progress 49 HM-032 - Drug Profile 54 Product Description 54 Mechanism Of Action 54 R&D Progress 54 LY-3023414 - Drug Profile 55 Product Description 55 Mechanism Of Action 55 R&D Progress 55 NSC-765844 - Drug Profile 57 Product Description 57 Mechanism Of Action 57 R&D Progress 57 omipalisib - Drug Profile 58 Product Description 58 Mechanism Of Action 58 R&D Progress 58 PQR-309 - Drug Profile 60 Product Description 60 Mechanism Of Action 60 R&D Progress 60 Small Molecule to Inhibit PI3K Alpha for Cancer - Drug Profile 63 Product Description 63 Mechanism Of Action 63 R&D Progress 63 Small Molecules to Inhibit Pan PI3K for Ovarian Cancer - Drug Profile 64 Product Description 64 Mechanism Of Action 64 R&D Progress 64 SPR-965 - Drug Profile 65 Product Description 65 Mechanism Of Action 65 R&D Progress 65 SRX-2523 - Drug Profile 66 Product Description 66 Mechanism Of Action 66 R&D Progress 66 TAK-117 - Drug Profile 68 Product Description 68 Mechanism Of Action 68 R&D Progress 68 taselisib - Drug Profile 70 Product Description 70 Mechanism Of Action 70 R&D Progress 70 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 Projects 72 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 74 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) - Featured News & Press Releases 75 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 75 Jun 02, 2016: Curis Announces Presentations Related to CUDC-907 at 2016 ASCO Annual Meeting 75 Apr 11, 2016: Curis Announces Presentation of Preclinical Data for CUDC-907 at AACR Annual Meeting 75 Apr 04, 2016: Curis Announces Publication of CUDC-907 Phase 1 Clinical Trial Data in Lancet Oncology 76 Jan 11, 2016: Seahorse Bioscience XF Technology Reaches 500th Citation in Cancer Research 76 Dec 06, 2015: Curis Reports Clinical Activity of CUDC-907 in Patients With DLBCL Harboring MYC Oncogene Alterations at the 2015 ASH Annual Meeting 77 Nov 05, 2015: Curis Announces Oral Presentation of Phase 1 Data for CUDC-907 at 2015 ASH Annual Meeting 79 Jun 17, 2015: Eli Lilly and Company Enters Into Strategic Partnership with Sarah Cannon Research Institute to Develop Investigational Oncology Therapy 80 Jun 10, 2015: Curis to Present CUDC-907 Clinical Data at the 20th Congress of the European Hematology Association and the 13th International Congress on Malignant Lymphoma 80 May 31, 2015: Curis Reports CUDC-907 Data From the Ongoing Phase 1 Trial at the 2015 ASCO Annual Meeting 81 May 27, 2015: PIQUR announces positive Phase 1 study results and the start of Phase 2 of PQR309 82 May 20, 2015: Curis Announces Presentations of CUDC-907 Clinical Data at 2015 ASCO Annual Meeting 83 May 10, 2015: New Investigational Drug Targeting Difficult to Treat Breast Cancers to Undergo Pan-European Phase II Clinical Trials 84 Apr 21, 2015: SignalRx Presents at 10th Annual Drug Discovery Chemistry Conference on its Dual Kinase-Epigenetic Inhibitors for Treating Cancer 85 Apr 17, 2015: PIQUR to present posters on its lead compound PQR309 at AACR Annual Meeting 2015 86 Appendix 88 Methodology 88 Coverage 88 Secondary Research 88 Primary Research 88 Expert Panel Validation 88 Contact Us 88 Disclaimer 89

List of Tables Number of Products under Development for, H2 2016 10 Number of Products under Development by Therapy Area, H2 2016 11 Number of Products under Development by Indication, H2 2016 13 Comparative Analysis by Late Stage Development, H2 2016 15 Comparative Analysis by Early Stage Products, H2 2016 16 Number of Products under Development by Companies, H2 2016 17 Products under Development by Companies, H2 2016 18 Products under Development by Companies, H2 2016 (Contd..1) 19 Products under Development by Companies, H2 2016 (Contd..2) 20 Products under Development by Companies, H2 2016 (Contd..3) 21 Products under Development by Companies, H2 2016 (Contd..4) 22 Number of Products under Investigation by Universities/Institutes, H2 2016 23 Products under Investigation by Universities/Institutes, H2 2016 24 Assessment by Monotherapy/Combination Products, H2 2016 25 Number of Products by Stage and Mechanism of Action, H2 2016 26 Number of Products by Stage and Route of Administration, H2 2016 27 Number of Products by Stage and Molecule Type, H2 2016 28 Pipeline by Bayer AG, H2 2016 29 Pipeline by Curis, Inc., H2 2016 30 Pipeline by Eli Lilly and Company, H2 2016 31 Pipeline by Genentech, Inc., H2 2016 32 Pipeline by GlaxoSmithKline Plc, H2 2016 33 Pipeline by Hutchison MediPharma Limited, H2 2016 34 Pipeline by Millennium Pharmaceuticals Inc, H2 2016 35 Pipeline by Novartis AG, H2 2016 36 Pipeline by PIQUR Therapeutics AG, H2 2016 38 Pipeline by Sphaera Pharma Pvt. Ltd., H2 2016 39 Dormant Projects, H2 2016 72 Dormant Projects (Contd..1), H2 2016 73 Discontinued Products, H2 2016 74 List of Figures Number of Products under Development for, H2 2016 10 Number of Products under Development by Therapy Area, H2 2016 11 Number of Products under Development by Top 10 Indication, H2 2016 12 Comparative Analysis by Late Stage Development, H2 2016 15 Comparative Analysis by Early Stage Products, H2 2016 16 Assessment by Monotherapy/Combination Products, H2 2016 25 Number of Products by Stage and Mechanism of Actions, H2 2016 26 Number of Products by Stage and Routes of Administration, H2 2016 27 Number of Products by Stage and Molecule Type, H2 2016 28

Bayer AG Curis, Inc. Eli Lilly and Company Genentech, Inc. GlaxoSmithKline Plc Hutchison MediPharma Limited Millennium Pharmaceuticals Inc Novartis AG PIQUR Therapeutics AG Sphaera Pharma Pvt. Ltd.