Full efficacy with no CNS side-effects: Unachievable panacea or reality? DMPK considerations in design of drugs with limited brain penetration

Xenobiotica

Volumn 42, Issue 1, 2012, Pages 11-27

  Cole, Susan ^a   Bagal, Sharan ^a   El Kattan, Ayman ^b   Fenner, Katherine ^a   Hay, Tanya ^a   Kempshall, Sarah ^a   Lunn, Graham ^a   Varma, Manthena ^b   Stupple, Paul ^a   Speed, William ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b PFIZER INC   (United States)

Author keywords

BCRP; Brain penetration; P gp; Peripheral restriction; Polar surface area

Indexed keywords

ABC TRANSPORTER; AMINO ACID TRANSPORTER; ATENOLOL; BACLOFEN; BREAST CANCER RESISTANCE PROTEIN; CARRIER PROTEIN; CETIRIZINE; FEXOFENADINE; GABAPENTIN; GLYCOPROTEIN P; HISTAMINE H3 RECEPTOR ANTAGONIST; IMATINIB; INDINAVIR; MELPHALAN; MONOCARBOXYLATE TRANSPORTER 1; NELFINAVIR; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 2; ORGANIC CATION TRANSPORTER 1; ORGANIC CATION TRANSPORTER 2; PEPTIDE TRANSPORTER 1; PF 3731237; PREGABALIN; PROTON DEPENDENT AMINO ACID TRANSPORTER; QUINIDINE; RITONAVIR; SAQUINAVIR; SODIUM MULTIVITAMIN TRANSPORTER; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ACTIVE TRANSPORT; ALLERGIC RHINITIS; BINDING AFFINITY; BLOOD BRAIN BARRIER; BRAIN INFECTION; CENTRAL NERVOUS SYSTEM; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG DIFFUSION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG METABOLISM; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SOLUBILITY; DRUG STRUCTURE; ELECTROENCEPHALOGRAM; HUMAN; INSOMNIA; INTESTINE CELL; LIPOPHILICITY; MEDICAL LITERATURE; MEMBRANE TRANSPORT; MOLECULAR SIZE; MOLECULAR WEIGHT; NEUROLOGIC DISEASE; NONHUMAN; PASSIVE TRANSPORT; PHOSPHOLIPID MEMBRANE; RECEPTOR OCCUPANCY; REVIEW; RISK REDUCTION; SURFACE PROPERTY; VIRUS INFECTION;

BLOOD-BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; DRUG COMPOUNDING; DRUG DISCOVERY; DRUG TOXICITY; HUMANS; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 82955168430     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2011.617847     Document Type: Review

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