Identification
NameAlectinib
Accession NumberDB11363
TypeSmall Molecule
GroupsApproved
Description

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It is specifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability.

Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance.

Structure
Thumb
Synonyms
9-ethyl-6,6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile
External IDs AF 802 / AF-802 / AF802 / CH 5424802 / CH-5424802 / CH5424802 / RO-5424802 / RO5424802
Product Ingredients
IngredientUNIICASInChI KeyDetails
Alectinib hydrochlorideP9YY73LO6J 1256589-74-8GYABBVHSRIHYJR-UHFFFAOYSA-NDetails
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlecensaCapsule150 mg/1OralGenentech, Inc.2015-12-11Not applicableUs
AlecensaroCapsule150 mgOralHoffmann La Roche2016-10-14Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIILIJ4CT1Z3Y
CAS numberNot Available
WeightAverage: 482.6166
Monoisotopic: 482.268176352
Chemical FormulaC30H34N4O2
InChI KeyKDGFLJKFZUIJMX-UHFFFAOYSA-N
InChI
InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3
IUPAC Name
9-ethyl-6,6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-5H,6H,11H-benzo[b]carbazole-3-carbonitrile
SMILES
CCC1=CC2=C(C=C1N1CCC(CC1)N1CCOCC1)C(C)(C)C1=C(C3=C(N1)C=C(C=C3)C#N)C2=O
Pharmacology
Indication

Alectinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This indication is approved under accelerated approval based on tumor response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.

Structured Indications
PharmacodynamicsNot Available
Mechanism of action

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It is specifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability. Both alectinib and its major active metabolite M4 demonstrate similar in vivo and in vitro activity against multiple mutant forms of ALK.

TargetKindPharmacological actionActionsOrganismUniProt ID
ALK tyrosine kinase receptorProteinyes
inhibitor
HumanQ9UM73 details
Related Articles
Absorption

Alectinib reached maximal concentrations at 4 hours following administration of 600 mg twice daily under fed conditions in patients with ALK-positive NSCLC. The absolute bioavailability was 37% in the fed state. A high-fat, high-calorie meal increased the combined exposure of alectinib and its major metabolite M4 by 3.1-fold following oral administration of a single 600 mg dose.

Volume of distribution

4016 L

Protein binding

Alectinib and its major metabolite M4 are >99% bound to human plasma proteins.

Metabolism

Alectinib is metabolized by CYP3A4 to its major active metabolite M4. M4 is then further metabolized by CYP3A4. Both alectinib and M4 demonstrate similar in vivo and in vitro activity. In vitro studies suggest that alectinib is not a substrate for P-gp while M4 is.

SubstrateEnzymesProduct
Alectinib
M4Details
M4
Metabolite 3Details
Route of elimination

When radioactively labeled, 98% of radioactivity was found in feces with 84% of that amount excreted as unchanged alectinib and 6% as M4. Less than 0.5% was found to be recovered in urine.

Half life

The mean elimination half life is 33 hr for alectinib and 31 hr for M4.

Clearance

The apparent clearance is 81.9L/hr for alectinib and 217 L/hr for M4.

Toxicity

The most common adverse reactions (>5%) associated with alectinib use were fatigue, constipation, edema, and myalgia. Less common effects associated with use were hepatotoxicity, interstitial lung disease (ILD)/pneumonitis, bradycardia, severe myalgia and creatine phosphokinase (CPK) elevation, and embryo-fetal toxicity. Females of reproductive potential are advised to use effective contraception during treatment with alectinib and for 1 week following the final dose.

Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Alectinib.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Alectinib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Alectinib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Alectinib.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Alectinib.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Alectinib.Approved, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Alectinib.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Alectinib.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Alectinib.Approved
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Alectinib.Approved, Investigational
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Alectinib.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Alectinib.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Alectinib.Approved, Investigational
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Alectinib.Approved, Vet Approved
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Alectinib.Withdrawn
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Alectinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Alectinib.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Alectinib.Approved, Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Alectinib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Alectinib.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Alectinib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Alectinib.Approved
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Alectinib.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Alectinib.Approved
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Alectinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Alectinib.Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Alectinib.Approved, Vet Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Alectinib.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Alectinib.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Alectinib.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Alectinib.Approved
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Alectinib.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Alectinib.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Alectinib.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Alectinib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Alectinib.Approved, Nutraceutical
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Alectinib.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Alectinib.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Alectinib.Approved
Conjugated estrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Alectinib.Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Alectinib.Approved
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Alectinib.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Alectinib.Approved
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Alectinib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Alectinib.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Alectinib.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Alectinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Alectinib.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Alectinib.Approved
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Alectinib.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Alectinib.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Alectinib.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Alectinib.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Alectinib.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Alectinib.Illicit
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Alectinib.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Alectinib.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Alectinib.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Alectinib.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Alectinib.Approved, Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Alectinib.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Alectinib.Approved, Investigational
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Alectinib.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Alectinib.Approved, Investigational
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Alectinib.Approved, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Alectinib.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Alectinib.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Alectinib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Alectinib.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Alectinib.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Alectinib.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Alectinib.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Alectinib.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Alectinib.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Alectinib.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Alectinib.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Alectinib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Alectinib.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Alectinib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Alectinib.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Alectinib.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Alectinib.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Alectinib.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Alectinib.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Alectinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Alectinib.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Alectinib.Approved
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Alectinib.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Alectinib.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Alectinib.Approved, Investigational
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Alectinib.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Alectinib.Approved
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Alectinib.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Alectinib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Alectinib.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Alectinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Alectinib.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Alectinib.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Alectinib.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Alectinib.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Alectinib.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Alectinib.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Alectinib.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Alectinib.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Alectinib.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Alectinib.Approved, Investigational
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Alectinib.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Alectinib.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Alectinib.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Alectinib.Approved, Illicit
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Alectinib.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Alectinib.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Alectinib.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Alectinib.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Alectinib.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Alectinib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Alectinib.Approved, Vet Approved
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Alectinib.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Alectinib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Alectinib.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Alectinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Alectinib.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Alectinib.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Alectinib.Approved, Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Alectinib.Approved
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Alectinib.Approved
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Alectinib.Approved, Vet Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Alectinib.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Alectinib.Approved
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Alectinib.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Alectinib.Approved, Vet Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Alectinib.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Alectinib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Alectinib.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Alectinib.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Alectinib.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Alectinib.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Alectinib.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Alectinib.Approved, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Alectinib.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Alectinib.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Alectinib.Approved
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Alectinib.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Alectinib.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Alectinib.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Alectinib.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Alectinib.Approved
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Alectinib.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Alectinib.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Alectinib.Approved, Investigational
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Alectinib.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Alectinib.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Alectinib.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Alectinib.Approved, Vet Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Alectinib.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Alectinib.Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Alectinib.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Alectinib.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Alectinib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Alectinib.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Alectinib.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Alectinib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Alectinib.Experimental
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Alectinib.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Alectinib.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Alectinib.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Alectinib.Approved
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Alectinib.Withdrawn
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Alectinib.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Alectinib.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Alectinib.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Alectinib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Alectinib.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Alectinib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Alectinib.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Alectinib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Alectinib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Alectinib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Alectinib.Approved
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Alectinib.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Alectinib.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Alectinib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Alectinib.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Alectinib.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Alectinib.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. McKeage K: Alectinib: a review of its use in advanced ALK-rearranged non-small cell lung cancer. Drugs. 2015 Jan;75(1):75-82. doi: 10.1007/s40265-014-0329-y. [PubMed:25428710 ]
  2. Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y: CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90. doi: 10.1016/j.ccr.2011.04.004. [PubMed:21575866 ]
  3. Kodama T, Tsukaguchi T, Yoshida M, Kondoh O, Sakamoto H: Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance. Cancer Lett. 2014 Sep 1;351(2):215-21. doi: 10.1016/j.canlet.2014.05.020. Epub 2014 Jun 2. [PubMed:24887559 ]
  4. Sullivan I, Planchard D: ALK inhibitors in non-small cell lung cancer: the latest evidence and developments. Ther Adv Med Oncol. 2016 Jan;8(1):32-47. doi: 10.1177/1758834015617355. [PubMed:26753004 ]
External Links
ATC CodesNot Available
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (581 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC) / Non-Squamous Non-Small Cell Lung Cancer1
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentHepatic Impairment1
1Unknown StatusTreatmentALK-Rearranged Non-Small Cell Lung Cancer1
1, 2Not Yet RecruitingTreatmentGlioblastoma, Adult1
1, 2RecruitingTreatmentALK-positive Non-small Cell Lung Cancer (NSCLC) / RET-positive Non-small Cell Lung Cancer (NSCLC) / RET-positive Thyroid Cancer1
1, 2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
2Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
2RecruitingTreatmentNeoplasms1
2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
2, 3Not Yet RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
3Active Not RecruitingTreatmentAnaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer / Non-Small-Cell Lung Carcinoma (NSCLC)1
3Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
3RecruitingTreatmentAnaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer1
3RecruitingTreatmentNeoplasms1
Not AvailableNo Longer AvailableNot AvailableNon-Small-Cell Lung Carcinoma (NSCLC)1
Not AvailableRecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral150 mg/1
CapsuleOral150 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9126931 No2011-05-292031-05-29Us
US9440922 No2010-06-092030-06-09Us
US9365514 No2012-03-042032-03-04Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
pKa7.05FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0105 mg/mLALOGPS
logP5.59ALOGPS
logP4.89ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)12.18ChemAxon
pKa (Strongest Basic)6.97ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area72.36 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity155.11 m3·mol-1ChemAxon
Polarizability56.45 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of chemical entities known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.
KingdomChemical entities
Super ClassOrganic compounds
ClassOrganoheterocyclic compounds
Sub ClassIndoles and derivatives
Direct ParentCarbazoles
Alternative ParentsNaphthalenes / Indoles / Aryl ketones / Dialkylarylamines / Aminopiperidines / Morpholines / Vinylogous amides / Heteroaromatic compounds / Pyrroles / Trialkylamines
SubstituentsCarbazole / Naphthalene / Indole / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Aryl ketone / 4-aminopiperidine / Morpholine / Oxazinane / Piperidine
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Neuronal orphan receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis and differentiation of the nervous system. Transduces signals from ligands at the cell surface, through specific activation of the mitogen-activated protein kinase (MAPK) pathway. Phosphorylates almost...
Gene Name:
ALK
Uniprot ID:
Q9UM73
Uniprot Name:
ALK tyrosine kinase receptor
Molecular Weight:
176440.535 Da

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Uniprot Name:
Multidrug resistance protein 1
Molecular Weight:
141477.255 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Uniprot Name:
ATP-binding cassette sub-family G member 2
Molecular Weight:
72313.47 Da
Drug created on January 19, 2016 12:11 / Updated on August 08, 2017 11:11