Sunday, 28 February 2016

Emicizumab



INN name:
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Emicizumab



Chemical name:
Immunoglobulin G4-kappa, bispecific, anti-[Homo sapiens F9a (activated coagulation factor F9, activated coagulation factor IX) and anti-[Homo sapiens F10 (coagulation factor 10, coagulation factor X)], humanized monoclonal antibody; gamma4 heavy chain (1-448) [humanized VH (Homo sapiens IGHV3-23*04 (87.80%) -(IGHD)-IGHJ4*01 (1- 123)), IGHG4*01 (CH1 K100>Q (202) (124-221), hinge S10>P (231) (222-233), CH2 F84.3>Y (299) (234-343), CH3 E12>K (359), R88>K (412), H115>R (438), L125>P (448) (344-448), CHS>del) (124-448)], (137-214')-disulfide with kappa light chain (1’-214’) [humanized V-KAPPA (Homo sapiens IGKV1-39*01 (80.00%) -IGKJ4*01) [6.3.9] (1'-107') -Homo sapiens IGKC*01, Km3 (108'-214')]; gamma4 heavy chain (1-444) [VH (Homo sapiens IGHV1- 2*02 (75.50%) -(IGHD)-IGHJ6*03 Q120>E (111''), T123>L (114'') (1''-119'')), IGHG4*01 (CH1 A100>Q (198'') (120''- 217''), hinge S10>P (227'') (218''-229''), CH2 F84.3>Y (295''), (230''-339''), CH3 R88>K (408), K119>E (438), L125>P (444) (340''-444''), CHS>del) (120''-444'')], (133''- 214''')-disulfide with kappa light chain (1'''-214''') [humanized V-KAPPA (Homo sapiens IGKV1-39*01 (80.00%) -IGKJ4*01) [6.3.9] (1'''-107''') -Homo sapiens IGKC*01, Km3 (108'''-214''')]; dimer (229-225":232-228")- bisdisulfide

Alternate Name:
Immunoglobulin G4-kappa, bispecific, anti-(homo sapiens F9a (activated coagulation factor F9, activated coagulation factor IX) and anti-(homo sapiens F10 (coagulation factor 10, coagulation factor X)), humanized monoclonal antibody


Heavy chain anti-F9a
QVQLVESGGG LVQPGGSLRL SCAASGFTFS YYDIQWVRQA PGKGLEWVSS 50
ISPSGQSTYY RREVKGRFTI SRDNSKNTLY LQMNSLRAED TAVYYCARRT 100
GREYGGGWYF DYWGQGTLVT VSSASTKGPS VFPLAPCSRS TSESTAALGC 150
LVKDYFPEPV TVSWNSGALT SGVHTFPAVL QSSGLYSLSS VVTVPSSSLG 200
TQTYTCNVDH KPSNTKVDKR VESKYGPPCP PCPAPEFLGG PSVFLFPPKP 250
KDTLMISRTP EVTCVVVDVS QEDPEVQFNW YVDGVEVHNA KTKPREEQYN 300
STYRVVSVLT VLHQDWLNGK EYKCKVSNKG LPSSIEKTIS KAKGQPREPQ 350
VYTLPPSQKE MTKNQVSLTC LVKGFYPSDI AVEWESNGQP ENNYKTTPPV 400
LDSDGSFFLY SKLTVDKSRW QEGNVFSCSV MHEALHNRYT QKSLSLSP 448
Heavy chain anti-F10
QVQLVQSGSE LKKPGASVKV SCKASGYTFT DNNMDWVRQA PGQGLEWMGD50
INTRSGGSIY NEEFQDRVIM TVDKSTDTAY MELSSLRSED TATYHCARRK 100
SYGYYLDEWG EGTLVTVSSA STKGPSVFPL APCSRSTSES TAALGCLVKD 150
YFPEPVTVSW NSGALTSGVH TFPAVLQSSG LYSLSSVVTV PSSSLGTQTY 200
TCNVDHKPSN TKVDKRVESK YGPPCPPCPA PEFLGGPSVF LFPPKPKDTL 250
MISRTPEVTC VVVDVSQEDP EVQFNWYVDG VEVHNAKTKP REEQYNSTYR 300
VVSVLTVLHQ DWLNGKEYKC KVSNKGLPSS IEKTISKAKG QPREPQVYTL 350
PPSQEEMTKN QVSLTCLVKG FYPSDIAVEW ESNGQPENNY KTTPPVLDSD 400
GSFFLYSKLT VDKSRWQEGN VFSCSVMHEA LHNHYTQESL SLSP 444
Light chain
DIQMTQSPSS LSASVGDRVT ITCKASRNIE RQLAWYQQKP GQAPELLIYQ 50
ASRKESGVPD RFSGSRYGTD FTLTISSLQP EDIATYYCQQ YSDPPLTFGG 100
GTKVEIKRTV AAPSVFIFPP SDEQLKSGTA SVVCLLNNFY PREAKVQWKV 150
DNALQSGNSQ ESVTEQDSKD STYSLSSTLT LSKADYEKHK VYACEVTHQG 200
LSSPVTKSFN RGEC
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Thursday, 4 February 2016

Alalevonadifloxacin

INN name:

Alalevonadifloxacin
Lab codes:

WCK-2349
Chemical name:

(5S)-8-[4-(L-alanyloxy)piperidin-1-yl]-9-fluoro-5-methyl-1-oxo-6,7-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid
Molecular formula:

C22H26FN3O5
Chemical Structure:

CAS Registry Number:

706809-20-3
Originator:

Wockhardt


Acebilustat

INN name:

Acebilustat
Lab codes:

CTX-4430
Chemical name:

4-{[(1S,4S)-5-({4-[4-(1,3-oxazol-2-yl)phenoxy]phenyl}methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]methyl}benzoic acid
Molecular formula:

C29H27N3O4
Chemical Structure:

CAS Registry Number:

943764-99-6
Originator:

Celtaxsys


Sunday, 11 October 2015

Evenamide

INN name:
Lab Code(s):
find at Drugspider
Chemical name:
2-{[2-(3-Butoxyphenyl)ethyl]amino}-N,N-dimethylacetamide
Chemical structure:
Molecular formula:
C16H26N2O2
CAS registry number:
1092977-61-1
Originator:
Newron Pharmaceuticals
Class:
Antidepressants
Antiepileptic drugs
Antimanics
Antipsychotics
Non-opioid analgesics
Mechanism of action:
Nav1.3 voltage-gated sodium channel inhibitors
Nav1.7-voltage-gated-sodium-channel-inhibitors
Nav1.8 voltage-gated sodium channel inhibitors
WHO ATC code(s):
N02 (Analgesics)
N03A (Antiepileptics)
N05A (Antipsychotics)
N05B (Anxiolytics)
N07X (Other Nervous System Drugs)
EPhMRA code(s):
N2 (Analgesics)
N3 (Anti-Epileptics)
N5A (Antipsychotics)
N5B (Hypnotics/Sedatives)
N6A (Anti-Depressants and Mood Stabilisers)
N7X (All other CNS drugs)
Clinical trial(s):
ConditionsPhasesInterventionsStatus
Safety and Tolerability in Healthy VolunteersPhase 1Drug: NW-3509aCompleted

Tuesday, 22 September 2015

Etripamil


INN name:
Etripamil

Lab codes:
find at Durgspider

Chemical name:
methyl 3-(2-{[(4S)-4-cyano-4-(3,4-dimethoxyphenyl)-
5-methylhexyl](methyl)amino}ethyl)benzoate

Molecular formula:
C27H36N2O4

Chemical Structure:
CAS Registry Number:
1593673-23-4


Originator:
Milestone Pharmaceuticals

Class:
Antiarrhythmics

Mechanism of Action:
Calcium channel antagonists

WHO ATC code:
C01 (Cardiac Therapy)
C01B (Antiarrhythmics, Class I and III)

EPhMRA code:
C1 (Cardiac Therapy)
C1B (Anti-Arrhythmics)

Clinical Trials:

Conditions
Phases
Status
Paroxysmal Supraventricular Tachycardia (PSVT)
Phase 2
Recruiting

Recent activities on the drug:

Guadecitabine


INN name:
Guadecitabine

Lab codes:
Decitabine deoxyguanosine; Decitabine deoxyguanosine dinucleotide; S-110; SGI-110

Chemical name:
2'-deoxy-5-azacytidylyl-(3'→5')-2'-deoxyguanosine
Molecular formula:
C18H24N9O10P

Chemical Structure:

CAS Registry Number:
929901-49-5

Originator:
SuperGen

Developer:
Astex Pharmaceuticals; Groupe Francophone des Myelodysplasies

Class:
Antineoplastics

Mechanism of Action:
Antimetabolites; DNA cytosine 5 methyltransferase 1 inhibitors

WHO ATC code:
L01B (Antimetabolites)

EPhMRA code:
L1B (Antimetabolites)

Clinical Trials:

Conditions
Phases
Status
Leukemia, Myeloid, Acute
Phase 3
Recruiting
Non-small Cell Lung Cancer
Phase 2
Completed
MDS
Phase 2
Recruiting
Hepatocellular Carcinoma
Phase 2
Active, not recruiting
Previously Treated Metastatic Colorectal Cancer
Phase 1 / Phase 2
Recruiting
MDS;   CMML;   AML
Phase 1 / Phase 2
Active, not recruiting
Ovarian Cancer
Phase 1 / Phase 2
Active, not recruiting
Germ Cell Tumor
Phase 1
Recruiting
Metastatic Colorectal Cancer
Phase 1
Recruiting
Acute Myeloid Leukemia
Phase 1
Recruiting

Recent activities on the drug:

Monday, 21 September 2015

Motolimod

INN name:

Motolimod
Lab codes:

VTX-2337

Chemical name:

2-amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzazepine-4-carboxamide

Molecular formula:

C28H34N4O2
Chemical Structure:


CAS Registry Number:

926927-61-9
Originator:

Array BioPharma
Developer:

VentiRx Pharmaceuticals
Class:

Antineoplastics, immunomodulator
Mechanism of Action:

Toll-like receptor 8 (TLR8) agonist
WHO ATC code:

L03A-X
EPhMRA code:

L3A9

Clinical Trials:

Conditions
Phases
Interventions
Recruitment
Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer
Phase 2
Combination
Active, not recruiting
Carcinoma, Squamous Cell of Head and Neck
Phase 2
Combination
Active, not recruiting
Ovarian Cancer
Phase 1|Phase 2
Combination
Not yet recruiting
Low Grade B Cell Lymphoma
Phase 1|Phase 2
Combination
Terminated
 Locally Advanced, Recurrent, or Metastatic Squamous Cell Cancer of Head and Neck
Phase 1
Combination
Completed
Recurrent or Persistent Ovarian Epithelial, Fallopian Tube, or Peritoneal Cavity Cancer
Phase 1
Combination
Completed
Squamous Cell Carcinoma of the Head and Neck
Phase 1
Combination
Recruiting
Advanced Solid Tumors|Lymphoma
Phase 1
Alone
Completed