500 New Molecular Entities in Clinical Development

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500 New Molecular Entities in Clinical Development

500 NEW MOLECULAR ENTITIES IN CLINICAL DEVELOPMENT

GENERIC NAME: ABEDITEROL

DEVELOPMENTAL CODE: LAS-100977

PHASE (08/2014): Clinical Phase II

STRUCTURE:

CAS NUMBER: 915133-65-2

MOLECULAR FORMULA: C25H30F2N2O4

IUPAC NAME: 5-[(1R)-2-[[6-(2,2-Difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl]-8-hydroxy-quinolin- 2(1H)-one

DRUG CLASS: Respiratory system drug

THERAPEUTIC CLAIM: Treatment of chronic obstructive pulmonary disease (COPD). The disease is, amongst others, a type of obstructive lung disease characterized by chronically poor airflow. It typically worsens over time. The main symptoms include breath shortness, cough and sputum production. People with chronic bronchitis often have COPD.

ACTIVITY / MOA: Adrenoreceptor agonist

COMPETING DRUGS*: Long acting β2-adrenergic receptor agonists, such as arformoterol (BROVANA®), bambuterol (BAMBEC®, OXEOL®), indacaterol (ONBREZ®, ARCAPTA®), procaterol (MEPTIN®), salmeterol

Short acting β2-adrenergic receptor agonists, such as fenoterol (BEROTEC®N), levalbuterol (XOPENEX®, LEVOLIN®), pirbuterol (MAXAIR®), salbutamol (VENTOLIN®), terbutalin (BRICANYL®)

Muscarinic receptor agonists, ipratropium bromide (ATROVENT®), tiotropium bromide (SPIRIVA®)

Glucocorticoids, such as fluticasone (FLIXOTIDE® / FLOVENT®), mometasone (NASONEX®), ciclesonide (ALVESCO®, MNARIS®)

Products from other classes, such as theophylline.

Combination drugs containing two actives from different classes are common.

DEVELOPMENT BY: ASTRA ZENECA p.l.c. (rights acquired from ALLMIRALL S.A., Spain) 500 NEW MOLECULAR ENTITIES IN CLINICAL DEVELOPMENT

DEVELOPMENTAL CODE: AP-26113

GENERIC NAME: na

PHASE (08/2014): Clinical Phase III

STRUCTURE:

CAS NUMBER: 1197958-12-5

MOLECULAR FORMULA: C26H34ClN6O2P

IUPAC NAME: (2-((5-Chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4- yl)amino)phenyl)dimethylphosphine oxide

DRUG CLASS: Antineoplastic and immunomodulating agents

THERAPEUTIC CLAIM: Potential treatment of non-small cell lung cancer and other forms of cancer

ACTIVITY / MOA: Inhibition of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR), resulting in inhibition of tumor cell growth.

COMPETING DRUGS*: Spindle disassembling inhibitors, such as cabazitaxel (JEVTANA®) and spindle assembling inhibitors, such as the vinca aldehydes vinblastine, vincristine, vinorelbine

DNA cross-linkers, such as bendamustine (e.g. TREANDA®), bleomycin, cyclophosphamide (ENDOXAN®), chlorambucil (LEUKERAN®), estramustine (ESTRACYT®), platinum containing drugs

Topomerase inhibitors, such as daunorubicin (MYOCET®), doxorubicin (DOXIL®/ CAELYX®), etoposide (VEPESID®), irinotecan (CAMPTOSAR®), mitoxantrone (NOVANTRONE®), topotecan (HYCAMTIN®)

Antimetabolites, such as capecitabine (XELODA®), gemcitabine (GEMZAR®), cytarabine, 5- fluorouracil, tegafur

Non classified drugs, such as eribulin (HALAVEN®).

DEVELOPMENT BY: ARIAD Inc.

ARIAD Inc., U.S.A.

BUSINESS: ARIAD Inc. is an American biopharmaceutical company focused on the development of oncological drugs, especially to treat lung cancer, leukemia and other difficult-to-treat cancers. The Company is headquartered in Cambridge, MA. 500 NEW MOLECULAR ENTITIES IN CLINICAL DEVELOPMENT

FINANCIALS: In US$ billion: 2014 2013 2012 2011 2010 Total Revenues: 0.05 0.00 0.03 0.18 Net profit: -0.27 -0.22 -0.01 0.09 Operating Income: -0.27 -0.21 -0.08 0.11 EBITDA: -0.27 -0.21 -0.07 0.11 Operating Cash Flow: -0.22 -0.15 -0.05 0.01 Net Profit Margin (%): neg neg neg neg Oper. CF margin (%): neg neg neg neg

MAIN ACTIVITIES: 100% Oncology

LARGEST PRODUCTS: As of today, the Company is not marketing any drugs

CONTACT ADDRESS: 26 Landsdowne Street Cambridge, MA 02139-4234, USA Phone: +1 (617) 494-0400 Fax: +1 (617) 494-8144 500 NEW MOLECULAR ENTITIES IN CLINICAL DEVELOPMENT

ASTRA ZENECA p.l.c., U.K.

BUSINESS: Astra Zeneca is the second largest British pharmaceutical company. The business comprises R&D, production and marketing of proprietary and licensed pharmaceuticals. The company was founded in 1999 by merging the pharmaceutical activities of Astra AB and ZENECA p.l.c.. Sales in North America accounted for 49% of AZ's total turnover, followed by Europe with 29% and all other markets with 22%.

In 2007, Astra Zeneca acquired US based biotech company MedImmune. several of AZ's pipeline products originate from MedImmune.

FINANCIALS: In US$ billion: 2014 2013 2012 2011 2010 Total Revenues: 25.71 27.97 33.51 33.27 Net profit: 2.57 6.33 10.02 8.08 Operating Income: 3.71 8.15 11.31 11.49 EBITDA: 8.30 10.67 15.34 14.24 Operating Cash Flow: 7.40 6.95 7.82 10.68 Net Profit Margin (%): 10.0 22.6 29.8 24.3 Oper. CF margin (%): 28.8 24.8 23.3 32.1

MAIN ACTIVITIES: 30% Cardiovascular 21% Neuroscience 16% Gastrointestinal 13% Respiratory & Inflammation 11 % Oncology 10% Others

LARGEST PRODUCTS: Rosuvastatin (CRESTOR®) Quetiapine (SEROQUEL®) Esomeprazol (NEXIUM®) Busedonide / Formeterol (SYMBICORT®) Candesartan (ATACAND®)

CONTACT ADDRESS: AstraZeneca PLC 2 Kingdom Street Paddington LondonW2 6BD Phone: +44 (0)20 7604 8000

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