Why obtaining a new drug amorphous form
The amorphous solid state possesses several advantages in comparison to the crystalline state which allow enhanced forms of drugs to be produced. Many drugs when generated as an amorphous form will exhibit one or more of the following: Solubility
The amorphous state is thermodynamically the form with the highest solubility. Consequently, amorphous forms will exhibit a greater solubility in a solvent than any crystalline form. Solubility advantages of factors >1000 have been observed between crystalline and amorphous drugs. The increased solubility of amorphous actives can lead to dramatically increased intrinsic dissolution rates when compared to crystalline forms. Activery offers the production of stable amorphous microparticles which show significantly enhanced solubility when compared to a crystalline reference.
Wettability
For a drug to dissolve, its surface has first to be wetted by the surrounding fluid. Amorphous forms possess a chemically randomized surface which expresses equal amounts of hydrophobic and hydrophilic interactions which can lead to improved wettability expressed by a lower contact angle a of the drug particle surface with a liquid. A lower contact angle represents a higher degree of hydrophily with consequently faster surface wetting and faster dissolution. Activery offers the generation of amorphous powders which show enhanced wetting through lower contact angles when compared to a crystalline starting material.
|
|
Brand Name(s)
|
Generic Name
|
Solid state
|
Sales 2006 (USD millions)
|
Change from 2005
|
Company(ies)
|
Disease/Medical Use
|
|
Lipitor
|
Atorvastatin
|
Non amorphous
|
14,385
|
7%
|
Pfizer, Astellas Pharma
|
Cholesterol
|
|
Advair, Seretide
|
Fluticasone + Salmeterol
|
Non amorphous
|
6,129
|
12%
|
GlaxoSmithKline
|
Asthma
|
|
Plavix, Iscover
|
Clopidogrel
|
Crystalline material
|
6,057
|
-5%
|
Bristol-Myers Squibb, Sanofi-Aventis
|
Thrombotic events
|
|
Nexium
|
Esomeprazole
|
Crystalline
|
5,182
|
12%
|
AstraZeneca
|
Gastrointestinal disorders
|
|
Norvasc
|
Amlodipine
|
Crystalline
|
4,866
|
3%
|
Pfizer
|
Hypertension
|
|
Remicade
|
Infliximab
|
Amorphous
|
4,428
|
23%
|
Johnson & Johnson, Schering-Plough, Tanabe
|
Rheumatoid arthritis
|
|
Enbrel
|
Etanercept
|
Amorphous
|
4,379
|
20%
|
Amgen, Wyeth
|
Rheumatoid arthritis
|
|
Zyprexa
|
Olanzapine
|
|
4,364
|
4%
|
Eli Lilly
|
Schizophrenia
|
|
Diovan
|
Valsartan
|
Amorphous drug
|
4,223
|
15%
|
Novartis
|
Hypertension
|
|
Risperdal
|
Risperidone
|
|
4,183
|
18%
|
Johnson & Johnson
|
Schizophrenia
|
|
Aranesp
|
Darbepoetin alfa
|
Amorphous
|
4,121
|
26%
|
Amgen
|
Anemia
|
|
Rituxan, MabThera
|
Rituximab
|
Amorphous
|
3,861
|
16%
|
Roche, Genentech, Biogen Idec, Chugai Pharmaceutical
|
Non-Hodgkin’s lymphoma
|
|
Effexor
|
Venlafaxine
|
Crystalline
|
3,722
|
8%
|
Wyeth
|
Depression, Anxiety disorders
|
|
Protonix, Pantozol, Pantoloc
|
Pantoprazole
|
Crystalline
|
3,621
|
4%
|
Wyeth, Altana, Solvay
|
Gastrointestinal disorders
|
|
Singulair
|
Montelukast
|
Crystalline
|
3,579
|
20%
|
Merck & Co.
|
Asthma
|
|
Seroquel
|
Quetiapine
|
Crystalline
|
3,560
|
23%
|
AstraZeneca, Astellas Pharma
|
Schizophrenia
|
|
Prevacid, Takepron
|
Lansoprazole
|
Crystalline
|
3,425
|
3%
|
TAP Pharmaceuticals, Takeda Pharmaceutical
|
Gastrointestinal disorders
|
|
Procrit, Eprex
|
Erythropoietin
|
Amorphous drug
|
3,180
|
-4%
|
Johnson & Johnson
|
Anemia
|
|
Cozaar, Hyzaar
|
Losartan
|
|
3,163
|
4%
|
Merck & Co.
|
Hypertension
|
|
Fosamax
|
Alendronate
|
|
3,134
|
-2%
|
Merck & Co.
|
Osteoporosis
|
|
Herceptin
|
Trastuzumab
|
Amorphous
|
3,134
|
83%
|
Roche, Genentech, Chugai Pharmaceutical
|
Breast cancer
|
|
Lovenox, Clexane
|
Enoxaparin
|
Amorphous
|
3,059
|
14%
|
Sanofi-Aventis
|
Deep-vein thrombosis
|
|
Avandia, Avandamet, Avandaryl
|
Rosiglitazone
|
Crystalline
|
3,043
|
26%
|
GlaxoSmithKline
|
Type 2 diabetes
|
|
Actos
|
Pioglitazone
|
Crystalline
|
2,880
|
25%
|
Takeda Pharmaceutical, Eli Lilly
|
Type 2 diabetes
|
|
Zocor
|
Simvastatin
|
Crystalline
|
2,803
|
-36%
|
Merck & Co.
|
Cholesterol
|
|
Copaxone
|
Glatiramer
|
Amorphous
|
2,757
|
19%
|
Teva Pharmaceutical Industries, Sanofi-Aventis
|
Multiple sclerosis
|
|
AcipHex, Pariet
|
Rabeprazole
|
Crystalline
|
2,729
|
-4%
|
Eisai, Johnson & Johnson
|
Gastrointestinal disorders
|
|
Neulasta
|
Filgrastim
|
Amorphous
|
2,710
|
18%
|
Amgen
|
Neutropenia
|
|
Lexapro, Cipralex
|
Escitalopram
|
Crystalline
|
2,696
|
16%
|
Forest Laboratories, H. Lundbeck
|
Depression, Anxiety disorders
|
|
Gleevec, Glivec
|
Imatinib
|
Non amorphous
|
2,554
|
18%
|
Novartis
|
Leukemia
|
|
Ambien, Stilnox
|
Zolpidem
|
Non amorphous
|
2,545
|
33%
|
Sanofi-Aventis
|
Insomnia
|
|
Aricept
|
Donepezil
|
Non amorphous
|
2,519
|
24%
|
Eisai, Pfizer
|
Alzheimer’s disease
|
|
Epogen
|
Erythropoietin
|
Amorphous
|
2,511
|
2%
|
Amgen
|
Anemia
|
|
Zyrtec, Cirrus
|
Cetirizine
|
Non amorphous
|
2,377
|
9%
|
Pfizer, UCB, Daiichi Sankyo
|
Allergic rhinitis
|
|
Avapro, Aprovel, Avalide
|
Irbesartan
|
Non amorphous
|
2,372
|
13%
|
Sanofi-Aventis, Bristol-Myers Squibb
|
Hypertension
|
|
Avastin
|
Bevacizumab
|
Amorphous
|
2,364
|
78%
|
Roche, Genentech
|
Colorectal cancer
|
|
Taxotere
|
Docetaxel
|
Amorphous
|
2,201
|
9%
|
Sanofi-Aventis
|
Cancer
|
|
Eloxatin, Eloxatine
|
Oxaliplatin
|
Amorphous
|
2,127
|
8%
|
Sanofi-Aventis
|
Colorectal cancer
|
|
Zoloft
|
Sertraline
|
Non amorphous
|
2,110
|
-35%
|
Pfizer
|
Depression, Anxiety disorders
|
|
Tamiflu
|
Oseltamivir
|
Non amorphous
|
2,096
|
69%
|
Roche, Chugai Pharmaceutical
|
Influenza
|
|
Lantus
|
Insulin analog
|
Amorphous
|
2,093
|
37%
|
Sanofi-Aventis
|
Type 2 diabetes and type 1 diabetes
|
|
Crestor
|
Rosuvastatin
|
Rosuvastatin calcium is a white amorphous powder
|
2,049
|
61%
|
AstraZeneca, Shionogi
|
Cholesterol
|
|
Humira
|
Adalimumab
|
Amorphous
|
2,044
|
46%
|
Abbott Laboratories
|
Rheumatoid arthritis
|
|
Celebrex
|
Celecoxib
|
Non amorphous
|
2,039
|
18%
|
Pfizer
|
Osteoarthritis and rheumatoid arthritis
|
|
Topamax
|
Topiramate
|
Non amorphous
|
2,027
|
21%
|
Johnson & Johnson
|
Seizures
|
|
Prevnar
|
vaccine
|
Amorphous
|
1,961
|
30%
|
Wyeth
|
Pneumococcal disease
|
|
Vytorin
|
Ezetimibe + Simvastatin
|
Non amorphous
|
1,955
|
90%
|
Merck & Co., Schering-Plough
|
Cholesterol
|
|
Zetia
|
Ezetimibe
|
Non amorphous
|
1,929
|
38%
|
Merck & Co., Schering-Plough
|
Cholesterol
|
|
Wellbutrin
|
Bupropion
|
Non amorphous
|
1,926
|
26%
|
GlaxoSmithKline, Biovail
|
Depression, Seasonal affective disorder (SAD)
|
|
Abilify
|
Aripiprazole
|
Crystalline
|
1,900
|
1%
|
Otsuka Pharmaceutical, Bristol-Myers Squibb
|
Schizophrenia
|
|
Lamictal
|
Lamotrigine
|
Crystalline
|
1,843
|
19%
|
GlaxoSmithKline
|
Seizures
|
|
Toprol, Seloken
|
Metoprolol
|
Crystalline
|
1,795
|
3%
|
AstraZeneca
|
Hypertension
|
|
NeoRecormon, Epogin
|
Erythropoietin
|
Amorphous
|
1,777
|
-1%
|
Roche, Chugai Pharmaceutical
|
Anemia
|
|
Atacand, Blopress
|
Candesartan
|
Cristalline
|
1,768
|
8%
|
Takeda Pharmaceutical, AstraZeneca
|
Hypertension
|
|
Spiriva
|
Tiotropium
|
Cristalline
|
1,735
|
45%
|
Boehringer Ingelheim
|
Chronic obstructive pulmonary disease
|
|
Avonex
|
Interferon beta-1a
|
Amorphous
|
1,707
|
11%
|
Biogen Idec
|
Multiple sclerosis
|
|
Viagra
|
Sildenafil
|
Crystalline
|
1,657
|
1%
|
Pfizer
|
Erectile dysfunction
|
|
Micardis
|
Telmisartan
|
Crystalline
|
1,645
|
35%
|
Boehringer Ingelheim, Astellas Pharma
|
Hypertension
|
|
Actonel
|
Risedronate
|
Crystalline
|
1,619
|
-4%
|
Procter & Gamble, Sanofi-Aventis
|
Osteoporosis
|
|
Lupron, Leuplin
|
Leuprolide
|
Amorphous
|
1,579
|
1%
|
Takeda Pharmaceutical, TAP Pharmaceuticals
|
Prostate cancer
|
|
TriCor, Lipanthyl
|
Fenofibrate
|
Amorphous
|
1,567
|
38%
|
Abbott Laboratories, Solvay
|
Cholesterol
|
|
Zofran
|
Ondansetron
|
Non amorphous
|
1,567
|
3%
|
GlaxoSmithKline
|
Nausea and vomiting
|
|
Valtrex
|
Valaciclovir
|
Non amorphous
|
1,563
|
24%
|
GlaxoSmithKline
|
Herpes
|
|
Levaquin, Floxin
|
Levofloxacin
|
Non amorphous
|
1,530
|
3%
|
Johnson & Johnson
|
Bacterial infections
|
|
Arimidex
|
Anastrozole
|
Non amorphous
|
1,508
|
28%
|
AstraZeneca
|
Breast cancer
|
|
Prograf
|
Tacrolimus
|
Non amorphous
|
1,499
|
20%
|
Astellas Pharma
|
Transplant rejection
|
|
CellCept
|
Mycophenolate mofetil
|
Non amorphous
|
1,470
|
8%
|
Roche, Chugai Pharmaceutical
|
Transplant rejection
|
|
Xalatan, Xalacom
|
Latanoprost
|
Non amorphous
|
1,453
|
6%
|
Pfizer
|
Intraocular pressure
|
|
Rebif
|
Interferon beta-1a
|
Amorphous
|
1,452
|
14%
|
Serono
|
Multiple sclerosis
|
|
Coreg
|
Carvedilol
|
Non amorphous
|
1,441
|
38%
|
GlaxoSmithKline
|
Hypertension
|
|
Gemzar
|
Gemcitabine
|
Non amorphous
|
1,408
|
5%
|
Eli Lilly
|
Cancer
|
|
Prilosec, Losec
|
Omeprazole
|
Non amorphous
|
1,371
|
-17%
|
AstraZeneca
|
Gastrointestinal disorders
|
|
Benicar, Olmetec
|
Olmesartan
|
Non amorphous
|
1,370
|
73%
|
Daiichi Sankyo, Forest Laboratories
|
Hypertension
|
|
Lotrel
|
Amlodipine + Benazepril
|
Non amorphous
|
1,352
|
26%
|
Novartis
|
Hypertension
|
|
Cymbalta
|
Duloxetine
|
Non amorphous
|
1,316
|
94%
|
Eli Lilly
|
Depression, Anxiety disorders
|
|
Imitrex, Imigran
|
Sumatriptan
|
Crystalline
|
1,315
|
4%
|
GlaxoSmithKline
|
Migraine
|
|
Depakote
|
Valproate semisodium
|
Crystalline
|
1,308
|
19%
|
Abbott Laboratories
|
Seizures
|
|
Humalog
|
Insulin analog
|
Crystalline
|
1,300
|
8%
|
Eli Lilly
|
Diabetes
|
|
Duragesic
|
Fentanyl
|
Crystalline
|
1,295
|
-18%
|
Johnson & Johnson
|
Pain
|
|
Pulmicort
|
Budesonide
|
Crystalline
|
1,292
|
11%
|
AstraZeneca
|
Asthma
|
|
Zometa
|
Zoledronate
|
Crystalline
|
1,283
|
5%
|
Novartis
|
Hypercalcemia
|
|
Betaseron, Betaferon
|
Interferon beta-1b
|
Amorphous
|
1,245
|
14%
|
Schering AG
|
Multiple sclerosis
|
|
Delix, Tritace
|
Ramipril
|
Crystalline
|
1,227
|
-3%
|
Sanofi-Aventis
|
Hypertension
|
|
Flovent, Flixotide
|
Fluticasone
|
Crystalline
|
1,219
|
5%
|
GlaxoSmithKline
|
Asthma
|
|
Neupogen
|
Filgrastim
|
Amorphous
|
1,213
|
0%
|
Amgen
|
Neutropenia
|
|
Casodex
|
Bicalutamide
|
Crystalline
|
1,206
|
7%
|
AstraZeneca
|
Prostate cancer
|
|
Pravachol
|
Pravastatin
|
Crystalline
|
1,197
|
-47%
|
Bristol-Myers Squibb
|
Cholesterol
|
|
Truvada
|
Tenofovir + Emtricitabine
|
Crystalline
|
1,194
|
110%
|
Gilead Sciences
|
HIV infection
|
|
Symbicort
|
Budesonide + Formoterol
|
Crystalline
|
1,184
|
18%
|
AstraZeneca
|
Asthma
|
|
Pegasys
|
Pegylated interferon alfa-2a
|
Amorphous
|
1,171
|
5%
|
Roche, Chugai Pharmaceutical
|
Hepatitis C
|
|
Evista
|
Raloxifene
|
Non-amorphous
|
1,159
|
4%
|
Eli Lilly, Chugai Pharmaceutical
|
Osteoporosis
|
|
Flomax
|
Tamsulosin
|
Crystalline
|
1,158
|
28%
|
Boehringer Ingelheim
|
Benign prostatic hypertrophy
|
|
Lyrica
|
Pregabalin
|
Crystalline
|
1,156
|
297%
|
Pfizer
|
Neuropathic pain
|
|
Paxil, Seroxat
|
Paroxetine
|
Crystalline
|
1,147
|
3%
|
GlaxoSmithKline
|
Depression, Anxiety disorders
|
|
Kaletra
|
Lopinavir
|
Crystalline
|
1,135
|
13%
|
Abbott Laboratories
|
HIV infection
|
|
Detrol
|
Tolterodine
|
Crystalline
|
1,100
|
11%
|
Pfizer
|
Overactive bladder
|
|
Harnal
|
Tamsulosin
|
Crystalline
|
1,085
|
-8%
|
Astellas Pharma
|
Benign prostatic hypertrophy
|
|
Erbitux
|
Cetuximab
|
Amorphous
|
1,075
|
56%
|
Bristol-Myers Squibb, Merck KGaA
|
Colorectal cancer
|
|
Synagis
|
Palivizumab
|
Amorphous
|
1,065
|
-9%
|
MedImmune
|
Respiratory syncytial virus
|
|
Augmentin
|
Co-amoxiclav
|
Crystalline
|
1,055
|
-13%
|
GlaxoSmithKline
|
Bacterial infections
|
|
Premarin, Prempro, Premphase
|
Estrogen
|
Crystalline
|
1,051
|
16%
|
Wyeth
|
Menopausal symptoms
|
|
Ortho contraceptives
|
Estrogen + Progesterone
|
Crystalline
|
1,016
|
-11%
|
Johnson & Johnson
|
Contraception
|
|
Zoladex
|
Goserelin
|
Amorphous
|
1,008
|
0%
|
AstraZeneca
|
Prostate cancer
|
|
Cerezyme
|
Imiglucerase
|
Amorphous
|
1,007
|
8%
|
Genzyme
|
Gaucher disease
|
|
Cravit
|
Levofloxacin
|
Crystalline
|
1,002
|
2%
|
Daiichi Sankyo, Santen Pharmaceutical
|
Bacterial infections
|
|
Yasmin
|
Drospirenone
|
Crystalline
|
998
|
36%
|
Schering AG
|
Prevention of pregnancy
|
|
Kogenate
|
Recombinant factor VIII
|
Amorphous
|
989
|
19%
|
Bayer
|
Hemophilia
|
|
Botox
|
Botulin toxin
|
Amorphous
|
982
|
18%
|
Allergan
|
Cervical dystonia
|
|
Lamisil
|
Terbinafine
|
Crystalline
|
978
|
-14%
|
Novartis
|
Fungal infections
|
|
Combivir
|
Lamivudine + Zidovudine
|
Crystalline
|
977
|
-8%
|
GlaxoSmithKline
|
HIV infection
|
|
Zosyn, Tazocin
|
Piperacillin
|
Crystalline
|
972
|
9%
|
Wyeth
|
Bacterial infections
|
|
Cialis
|
Tadalafil
|
Crystalline
|
971
|
30%
|
Lilly, Lilly Icos
|
Erectile dysfunction
|
|
Keppra
|
Levetiracetam
|
|
956
|
36%
|
UCB
|
Seizures
|
|
NovoSeven
|
Factor VII
|
Amorphous
|
948
|
11%
|
Novo Nordisk
|
Bleeding due to hemophilia
|
|
Infanrix, Pediarix
|
vaccine
|
Amorphous
|
945
|
21%
|
GlaxoSmithKline
|
Diphtheria, tetanus, and pertussis
|
|
Nasonex
|
Mometasone
|
Non-amorphous
|
944
|
28%
|
Schering-Plough
|
Allergic rhinitis
|
|
Reyataz
|
Atazanavir
|
Non-amorphous
|
931
|
34%
|
Bristol-Myers Squibb
|
HIV infection
|
|
Concerta
|
Methylphenidate
|
Non-amorphous
|
930
|
20%
|
Johnson & Johnson
|
Attention-deficit hyperactivity disorder
|
|
Humulin
|
Recombinant human insulin
|
Amorphous
|
925
|
-8%
|
Eli Lilly
|
Diabetes
|
|
Neoral, Sandimmun
|
Ciclosporin
|
Amorphous
|
918
|
-4%
|
Novartis
|
Transplant rejection
|
|
Sandostatin
|
Somatostatin
|
Amorphous
|
915
|
2%
|
Novartis
|
Acromegaly
|
|
Camptosar
|
Irinotecan
|
Amorphous
|
903
|
-1%
|
Pfizer
|
Colorectal cancer
|
|
Engerix-B, Havrix, Twinrix
|
vaccine
|
Amorphous
|
886
|
10%
|
GlaxoSmithKline
|
Hepatitis
|
|
Allegra, Telfast
|
Fexofenadine
|
Non-amorphous
|
864
|
-49%
|
Sanofi-Aventis
|
Allergic rhinitis
|
|
Adderall
|
Amphetamine
|
Non-amorphous
|
864
|
18%
|
Shire Pharmaceuticals
|
Attention-deficit hyperactivity disorder
|
|
Combivent
|
Ipratropium + Salbutamol
|
Non-amorphous
|
843
|
20%
|
Boehringer Ingelheim
|
Chronic obstructive pulmonary disease
|
|
Peg-Intron
|
Pegylated interferon alfa-2b
|
Amorphous
|
837
|
11%
|
Schering-Plough
|
Hepatitis C
|
|
Adalat
|
Nifedipine
|
Non-amorphous
|
825
|
0%
|
Bayer
|
Hypertension
|
|
Avelox, Avalox
|
Moxifloxacin
|
Non-amorphous
|
822
|
17%
|
Bayer, Schering-Plough, Shionogi
|
Bacterial infections
|
|
Mobic
|
Meloxicam
|
Non-amorphous
|
818
|
-66%
|
Boehringer Ingelheim, Daiichi Sankyo
|
Osteoarthritis and rheumatoid arthritis
|
|
Biaxin
|
Clarithromycin
|
Non-amorphous
|
816
|
-23%
|
Abbott Laboratories
|
Bacterial infections
|
|
Mevalotin
|
Pravastatin
|
Non-amorphous
|
799
|
-35%
|
Daiichi Sankyo
|
Cholesterol
|
|
Ultane, Sevorane
|
Sevoflurane
|
Amorphous
|
799
|
-9%
|
Abbott Laboratories
|
Anesthesia
|
|
Genotropin
|
Somatropin
|
Amorphous
|
795
|
-2%
|
Pfizer
|
Growth failure
|
|
Sustiva
|
Efavirenz
|
Crystalline
|
791
|
16%
|
Bristol-Myers Squibb
|
HIV infection
|
|
Zyvox
|
Linezolid
|
Crystalline
|
782
|
27%
|
Pfizer
|
Bacterial infections
|
|
Xeloda
|
Capecitabine
|
Crystalline
|
775
|
22%
|
Roche, Chugai Pharmaceutical
|
Cancer
|
|
Geodon, Zeldox
|
Ziprasidone
|
Crystalline
|
758
|
29%
|
Pfizer
|
Schizophrenia
|
|
Cipro, Ciprobay
|
Ciprofloxacin
|
Crystalline
|
755
|
-6%
|
Bayer, Schering-Plough
|
Bacterial infections
|
|
Provigil
|
Modafinil
|
Crystalline
|
735
|
43%
|
Cephalon
|
Sleepiness
|
|
Lescol
|
Fluvastatin
|
Crystalline
|
725
|
-5%
|
Novartis
|
Cholesterol
|
|
Clarinex, Aerius
|
Desloratadine
|
Crystalline
|
722
|
12%
|
Schering-Plough
|
Allergic rhinitis
|
|
Femara
|
Letrozole
|
Crystalline
|
722
|
35%
|
Novartis, Chugai Pharmaceutical
|
Breast cancer
|
|
Trileptal
|
Oxcarbazepine
|
Crystalline
|
721
|
17%
|
Novartis
|
Seizures
|
|
Tracleer
|
Bosentan
|
|
717
|
42%
|
Actelion
|
Pulmonary arterial hypertension
|
|
Primaxin
|
Imipenem + Cilastatin
|
Amorphous
|
705
|
-5%
|
Merck & Co.
|
Bacterial infections
|
|
Temodar
|
Temozolomide
|
Crystalline
|
703
|
20%
|
Schering-Plough
|
Anaplastic astrocytoma
|
|
Trusopt, Cosopt
|
Dorzolamide
|
Crystalline
|
697
|
13%
|
Merck & Co.
|
Intraocular pressure
|
|
Voltaren
|
Diclofenac
|
Crystalline
|
690
|
0%
|
Novartis
|
Osteoarthritis and rheumatoid arthritis
|
|
Viread
|
Tenofovir
|
Crystalline
|
689
|
-12%
|
Gilead Sciences
|
HIV infection
|
|
Sifrol
|
Pramipexole
|
Crystalline
|
673
|
23%
|
Boehringer Ingelheim
|
Parkinson’s disease
|
|
Namenda
|
Memantine
|
Crystalline
|
660
|
30%
|
Forest Laboratories
|
Alzheimer disease
|
|
Altace
|
Ramipril
|
Crystalline
|
653
|
18%
|
King Pharmaceuticals
|
Cardiovascular events
|
|
Byetta
|
Exenatide
|
Amorphous
|
649
|
464%
|
Amylin Pharmaceuticals, Eli Lilly
|
Type 2 diabetes
|
|
Tarceva
|
Erlotinib
|
Crystalline
|
649
|
110%
|
Roche, Genentech
|
Non-small cell lung cancer
|
|
Zithromax, Zmax
|
Azithromycin
|
Crystalline
|
638
|
-68%
|
Pfizer
|
Bacterial infections
|
|
Omnicef
|
Cefdinir
|
Amorphous
|
637
|
29%
|
Abbott Laboratories
|
Bacterial infections
|
|
Proscar
|
Finasteride
|
Crystalline
|
619
|
-16%
|
Merck & Co.
|
Benign prostatic hypertrophy
|
|
Alimta
|
Pemetrexed
|
Amorphous
|
612
|
32%
|
Eli Lilly
|
Non-small cell lung cancer
|
|
Merrem
|
Meropenem
|
|
604
|
20%
|
AstraZeneca
|
Bacterial infections
|
|
Forteo
|
Teriparatide
|
Amorphous
|
594
|
53%
|
Eli Lilly
|
Osteoporosis
|
|
Strattera
|
Atomoxetine
|
Crystalline
|
579
|
5%
|
Eli Lilly
|
Attention-deficit hyperactivity disorder
|
|
Actiq
|
Fentanyl
|
Crystalline
|
578
|
40%
|
Cephalon
|
Cancer pain
|
|
Flonase, Flixonase
|
Fluticasone
|
Crystalline
|
575
|
-52%
|
GlaxoSmithKline
|
Allergic rhinitis
|
|
Amaryl
|
Glimepiride
|
Crystalline
|
567
|
-33%
|
Sanofi-Aventis
|
Type 2 diabetes
|
|
Lidoderm
|
Lidocaine
|
Amorphous
|
567
|
35%
|
Endo Pharmaceuticals
|
Pain
|
|
Lunesta
|
Eszopiclone
|
Non amorphous
|
567
|
72%
|
Sepracor
|
Insomnia
|
|
Boniva, Bonviva
|
Ibandronate
|
Non amorphous
|
565
|
454%
|
Roche, GlaxoSmithKline
|
Osteoporosis
|
|
Taxol
|
Paclitaxel
|
Amorphous
|
563
|
-25%
|
Bristol-Myers Squibb
|
Cancer
|
|
Zelnorm, Zelmac
|
Tegaserod
|
Non amorphous
|
561
|
34%
|
Novartis
|
Irritable bowel syndrome
|
|
Renagel
|
Sevelamer
|
Non amorphous
|
559
|
23%
|
Genzyme, Roche, Chugai Pharmaceutical
|
Hyperphosphatemia
|
|
Norditropin
|
Human growth hormone
|
Amorphous
|
557
|
19%
|
Novo Nordisk
|
Growth hormone deficiency
|
|
Xopenex
|
Levalbuterol
|
Non amorphous
|
555
|
29%
|
Sepracor
|
Bronchospasm
|
|
Xenical
|
Orlistat
|
Non amorphous
|
553
|
9%
|
Roche
|
Obesity
|
|
Vasotec, Vaseretic
|
Enalapril
|
Non amorphous
|
547
|
-12%
|
Merck & Co.
|
Hypertension
|
|
Serevent
|
Salmeterol
|
Non amorphous
|
538
|
-10%
|
GlaxoSmithKline
|
Asthma
|
|
Cardura
|
Doxazosin
|
Non amorphous
|
538
|
-8%
|
Pfizer
|
Hypertension
|
|
Synthroid
|
Levothyroxine
|
Non amorphous
|
534
|
-4%
|
Abbott Laboratories
|
Hypothyroidism
|
|
Gonal-f
|
Follitropin alfa
|
Amorphous
|
533
|
-3%
|
Serono
|
Infertility
|
|
Gaster
|
Famotidine
|
|
532
|
-10%
|
Astellas Pharma
|
Gastrointestinal disorders
|
|
Cancidas
|
Caspofungin
|
Amorphous
|
530
|
-7%
|
Merck & Co.
|
Fungal infections
|
|
Exelon
|
Rivastigmine
|
Non amorphous
|
525
|
12%
|
Novartis
|
Alzheimer’s disease
|
|
Vfend
|
Voriconazole
|
Non amorphous
|
515
|
30%
|
Pfizer
|
Fungal infections
|
|
Amlodin
|
Amlodipine
|
Non amorphous
|
506
|
4%
|
Dainippon Sumitomo
|
Hypertension, angina pectoris
|
|
Niaspan
|
Niacin
|
Non amorphous
|
498
|
13%
|
Kos Pharmaceuticals
|
Cholesterol
|
|
Neurontin
|
Gabapentin
|
Non amorphous
|
496
|
-22%
|
Pfizer
|
Seizures
|
|
Trizivir
|
Abacavir + Lamivudine + Zidovudine
|
Non amorphous
|
496
|
-10%
|
GlaxoSmithKline
|
HIV infection
|
|
Requip
|
Ropinirole
|
Non amorphous
|
496
|
74%
|
GlaxoSmithKline
|
Parkinson disease
|
|
Follistim, Puregon
|
Follitropin beta
|
Amorphous
|
482
|
8%
|
Akzo Nobel
|
Infertility
|
|
Basen
|
Voglibose
|
Non amorphous
|
476
|
-13%
|
Takeda Pharmaceutical
|
Hyperglycemia
|
|
Levitra
|
Vardenafil
|
Non amorphous
|
474
|
19%
|
Bayer, GlaxoSmithKline
|
Erectile dysfunction
|
|
Glucophage
|
Metformin
|
Non amorphous
|
459
|
-16%
|
Merck KGaA, Bristol-Myers Squibb
|
Type 2 diabetes
|
|
Concor
|
Bisoprolol
|
Non amorphous
|
455
|
4%
|
Merck KGaA
|
Hypertension
|
|
Epzicom, Kixeva
|
Abacavir + Lamivudine
|
Non amorphous
|
446
|
107%
|
GlaxoSmithKline
|
HIV infection
|
|
Xatral
|
Alfuzosin
|
Crystalline
|
443
|
8%
|
Sanofi-Aventis
|
Benign prostatic hypertrophy
|
|
Diflucan
|
Fluconazole
|
Crystalline
|
435
|
-13%
|
Pfizer
|
Fungal infections
|
|
Thalomid
|
Thalidomide
|
Crystalline
|
433
|
12%
|
Celgene
|
Erythema nodosum leprosum
|
|
Zantac
|
Ranitidine
|
Crystalline
|
429
|
-18%
|
GlaxoSmithKline
|
Gastrointestinal disorders
|
|
Xolair
|
Omalizumab
|
Amorphous
|
429
|
32%
|
Roche, Genentech
|
Asthma
|
|
Claritin
|
Loratadine
|
Crystalline
|
418
|
-5%
|
Schering-Plough, Shionogi & Co.
|
Allergic rhinitis
|
|
|
|