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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Alectinib
- Accession Number
- DB11363
- Type
- Small Molecule
- Groups
- Approved
- 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
Structure for DB11363 (Alectinib)
- 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
Ingredient UNII CAS InChI Key Alectinib hydrochloride P9YY73LO6J 1256589-74-8 GYABBVHSRIHYJR-UHFFFAOYSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Alecensa Capsule 150 mg/1 Oral Genentech, Inc. 2015-12-11 Not applicable US 
Alecensaro Capsule 150 mg Oral Hoffmann La Roche 2016-10-14 Not applicable Canada 
- Categories
- UNII
- LIJ4CT1Z3Y
- CAS number
- Not Available
- Weight
- Average: 482.6166
Monoisotopic: 482.268176352 - Chemical Formula
- C30H34N4O2
- InChI Key
- KDGFLJKFZUIJMX-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
- Pharmacodynamics
- Not 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.
Target Actions Organism AALK tyrosine kinase receptor inhibitorHuman - 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.
Reactions:
- 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 organisms
- Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Acebutolol The serum concentration of Acebutolol can be increased when it is combined with Alectinib. Approved Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Alectinib. Approved Acetylsalicylic acid The serum concentration of Acetylsalicylic acid can be increased when it is combined with Alectinib. Approved, Vet Approved Afatinib The serum concentration of Afatinib can be increased when it is combined with Alectinib. Approved Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Alectinib. Experimental Alitretinoin The serum concentration of Alitretinoin can be increased when it is combined with Alectinib. Approved, Investigational Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Alectinib. Approved, Investigational Amitriptyline The serum concentration of Amitriptyline can be increased when it is combined with Alectinib. Approved Apixaban The serum concentration of Apixaban can be increased when it is combined with Alectinib. Approved Arsenic trioxide The serum concentration of Arsenic trioxide can be increased when it is combined with Alectinib. Approved, Investigational Atazanavir The serum concentration of Atazanavir can be increased when it is combined with Alectinib. Approved, Investigational Atenolol The serum concentration of Atenolol can be increased when it is combined with Alectinib. Approved Axitinib The serum concentration of Axitinib can be increased when it is combined with Alectinib. Approved, Investigational Belinostat The serum concentration of Belinostat can be increased when it is combined with Alectinib. Approved, Investigational Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Alectinib. Approved, Vet Approved Boceprevir The serum concentration of Boceprevir can be increased when it is combined with Alectinib. Withdrawn Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Alectinib. Approved Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Alectinib. Approved Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Alectinib. Approved, Investigational Cabazitaxel The serum concentration of Cabazitaxel can be increased when it is combined with Alectinib. Approved Caffeine The serum concentration of Caffeine can be increased when it is combined with Alectinib. Approved Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Alectinib. Experimental Canagliflozin The serum concentration of Canagliflozin can be increased when it is combined with Alectinib. Approved Carbamazepine The serum concentration of Carbamazepine can be increased when it is combined with Alectinib. Approved, Investigational Carfilzomib The serum concentration of Carfilzomib can be increased when it is combined with Alectinib. Approved Ceritinib The serum concentration of Ceritinib can be increased when it is combined with Alectinib. Approved Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Alectinib. Withdrawn Chlorpromazine The serum concentration of Chlorpromazine can be increased when it is combined with Alectinib. Approved, Vet Approved Cimetidine The serum concentration of Cimetidine can be increased when it is combined with Alectinib. Approved Ciprofloxacin The serum concentration of Ciprofloxacin can be increased when it is combined with Alectinib. Approved, Investigational Cisplatin The serum concentration of Cisplatin can be increased when it is combined with Alectinib. Approved Citalopram The serum concentration of Citalopram can be increased when it is combined with Alectinib. Approved Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Alectinib. Approved Clobazam The serum concentration of Clobazam can be increased when it is combined with Alectinib. Approved, Illicit Clomifene The serum concentration of Clomifene can be increased when it is combined with Alectinib. Approved, Investigational Clonidine The serum concentration of Clonidine can be increased when it is combined with Alectinib. Approved Clopidogrel The serum concentration of Clopidogrel can be increased when it is combined with Alectinib. Approved, Nutraceutical Clozapine The serum concentration of Clozapine can be increased when it is combined with Alectinib. Approved Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Alectinib. Approved Colchicine The serum concentration of Colchicine can be increased when it is combined with Alectinib. Approved Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Alectinib. Approved Copanlisib The serum concentration of Copanlisib can be increased when it is combined with Alectinib. Approved Crizotinib The serum concentration of Crizotinib can be increased when it is combined with Alectinib. Approved Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Alectinib. Approved, Investigational, Vet Approved Dabigatran etexilate The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Alectinib. Approved Dabrafenib The serum concentration of Dabrafenib can be increased when it is combined with Alectinib. Approved Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Alectinib. Approved Dapagliflozin The serum concentration of Dapagliflozin can be increased when it is combined with Alectinib. Approved Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Alectinib. Approved, Investigational Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Alectinib. Approved Debrisoquin The serum concentration of Debrisoquin can be increased when it is combined with Alectinib. Approved Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Alectinib. Approved, Investigational, Vet Approved Diazepam The serum concentration of Diazepam can be increased when it is combined with Alectinib. Approved, Illicit, Vet Approved Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Alectinib. Approved Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Alectinib. Approved Digoxin The serum concentration of Digoxin can be increased when it is combined with Alectinib. Approved Dihydrotestosterone The serum concentration of Dihydrotestosterone can be increased when it is combined with Alectinib. Illicit Diltiazem The serum concentration of Diltiazem can be increased when it is combined with Alectinib. Approved Dipyridamole The serum concentration of Dipyridamole can be increased when it is combined with Alectinib. Approved Docetaxel The serum concentration of Docetaxel can be increased when it is combined with Alectinib. Approved, Investigational Domperidone The serum concentration of Domperidone can be increased when it is combined with Alectinib. Approved, Investigational, Vet Approved Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Alectinib. Approved, Investigational Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Alectinib. Approved Elbasvir The serum concentration of Elbasvir can be increased when it is combined with Alectinib. Approved Eletriptan The serum concentration of Eletriptan can be increased when it is combined with Alectinib. Approved, Investigational Enasidenib The serum concentration of Enasidenib can be increased when it is combined with Alectinib. Approved Epinastine The serum concentration of Epinastine can be increased when it is combined with Alectinib. Approved, Investigational Erlotinib The serum concentration of Erlotinib can be increased when it is combined with Alectinib. Approved, Investigational Erythromycin The serum concentration of Erythromycin can be increased when it is combined with Alectinib. Approved, Vet Approved Estradiol The serum concentration of Estradiol can be increased when it is combined with Alectinib. Approved, Investigational, Vet Approved Estriol The serum concentration of Estriol can be increased when it is combined with Alectinib. Approved, Vet Approved Estrone The serum concentration of Estrone can be increased when it is combined with Alectinib. Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be increased when it is combined with Alectinib. Approved Etoposide The serum concentration of Etoposide can be increased when it is combined with Alectinib. Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Alectinib. Approved Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Alectinib. Approved Fesoterodine The serum concentration of Fesoterodine can be increased when it is combined with Alectinib. Approved Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Alectinib. Approved Fidaxomicin The serum concentration of Fidaxomicin can be increased when it is combined with Alectinib. Approved Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Alectinib. Approved Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Alectinib. Approved, Investigational Gemcitabine The serum concentration of Gemcitabine can be increased when it is combined with Alectinib. Approved Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Alectinib. Approved Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Alectinib. Approved Grepafloxacin The serum concentration of Grepafloxacin can be increased when it is combined with Alectinib. Withdrawn Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Alectinib. Approved Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Alectinib. Approved, Vet Approved Ibuprofen The serum concentration of Ibuprofen can be increased when it is combined with Alectinib. Approved Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Alectinib. Approved Imatinib The serum concentration of Imatinib can be increased when it is combined with Alectinib. Approved Imipramine The serum concentration of Imipramine can be increased when it is combined with Alectinib. Approved Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Alectinib. Approved Indinavir The serum concentration of Indinavir can be increased when it is combined with Alectinib. Approved Indomethacin The serum concentration of Indomethacin can be increased when it is combined with Alectinib. Approved, Investigational Inotuzumab ozogamicin The serum concentration of Inotuzumab ozogamicin can be increased when it is combined with Alectinib. Approved Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Alectinib. Approved, Investigational Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Alectinib. Approved, Vet Approved Ketazolam The serum concentration of Ketazolam can be increased when it is combined with Alectinib. Approved Ketoconazole The serum concentration of Ketoconazole can be increased when it is combined with Alectinib. Approved, Investigational Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Alectinib. Approved, Investigational Lamotrigine The serum concentration of Lamotrigine can be increased when it is combined with Alectinib. Approved, Investigational Lansoprazole The serum concentration of Lansoprazole can be increased when it is combined with Alectinib. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Alectinib. Approved Lenalidomide The serum concentration of Lenalidomide can be increased when it is combined with Alectinib. Approved Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Alectinib. Approved Levetiracetam The serum concentration of Levetiracetam can be increased when it is combined with Alectinib. Approved, Investigational Levofloxacin The serum concentration of Levofloxacin can be increased when it is combined with Alectinib. Approved, Investigational Levomilnacipran The serum concentration of Levomilnacipran can be increased when it is combined with Alectinib. Approved Linagliptin The serum concentration of Linagliptin can be increased when it is combined with Alectinib. Approved Loperamide The serum concentration of Loperamide can be increased when it is combined with Alectinib. Approved Losartan The serum concentration of Losartan can be increased when it is combined with Alectinib. Approved Mannitol The serum concentration of Mannitol can be increased when it is combined with Alectinib. Approved, Investigational Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Alectinib. Approved Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Alectinib. Approved, Vet Approved Metoprolol The serum concentration of Metoprolol can be increased when it is combined with Alectinib. Approved, Investigational Midazolam The serum concentration of Midazolam can be increased when it is combined with Alectinib. Approved, Illicit Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Alectinib. Approved Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Alectinib. Approved, Investigational Morphine The serum concentration of Morphine can be increased when it is combined with Alectinib. Approved, Investigational Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Alectinib. Approved, Investigational Nadolol The serum concentration of Nadolol can be increased when it is combined with Alectinib. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Alectinib. Approved Naloxone The serum concentration of Naloxone can be increased when it is combined with Alectinib. Approved, Vet Approved Nelfinavir The serum concentration of Nelfinavir can be increased when it is combined with Alectinib. Approved Nicardipine The serum concentration of Nicardipine can be increased when it is combined with Alectinib. Approved Nifedipine The serum concentration of Nifedipine can be increased when it is combined with Alectinib. Approved Nilotinib The serum concentration of Nilotinib can be increased when it is combined with Alectinib. Approved, Investigational Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Alectinib. Approved Nizatidine The serum concentration of Nizatidine can be increased when it is combined with Alectinib. Approved Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Alectinib. Investigational Olanzapine The serum concentration of Olanzapine can be increased when it is combined with Alectinib. Approved, Investigational Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Alectinib. Approved Osimertinib The serum concentration of Osimertinib can be increased when it is combined with Alectinib. Approved Paclitaxel The serum concentration of Paclitaxel can be increased when it is combined with Alectinib. Approved, Vet Approved Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Alectinib. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Alectinib. Approved Phenobarbital The serum concentration of Phenobarbital can be increased when it is combined with Alectinib. Approved Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Alectinib. Approved, Vet Approved Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Alectinib. Approved Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Alectinib. Approved Pomalidomide The serum concentration of Pomalidomide can be increased when it is combined with Alectinib. Approved Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Alectinib. Approved Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Alectinib. Approved Prazosin The serum concentration of Prazosin can be increased when it is combined with Alectinib. Approved Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Alectinib. Approved, Vet Approved Prednisone The serum concentration of Prednisone can be increased when it is combined with Alectinib. Approved, Vet Approved Progesterone The serum concentration of Progesterone can be increased when it is combined with Alectinib. Approved, Vet Approved Propranolol The serum concentration of Propranolol can be increased when it is combined with Alectinib. Approved, Investigational Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Alectinib. Approved Quetiapine The serum concentration of Quetiapine can be increased when it is combined with Alectinib. Approved Quinidine The serum concentration of Quinidine can be increased when it is combined with Alectinib. Approved Quinine The serum concentration of Quinine can be increased when it is combined with Alectinib. Approved Ranitidine The serum concentration of Ranitidine can be increased when it is combined with Alectinib. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Alectinib. Approved, Investigational Reserpine The serum concentration of Reserpine can be increased when it is combined with Alectinib. Approved Rifampicin The serum concentration of Rifampicin can be increased when it is combined with Alectinib. Approved Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Alectinib. Approved, Investigational Risperidone The serum concentration of Risperidone can be increased when it is combined with Alectinib. Approved, Investigational Ritonavir The serum concentration of Ritonavir can be increased when it is combined with Alectinib. Approved, Investigational Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Alectinib. Approved Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Alectinib. Approved, Investigational Salicylic acid The serum concentration of Salicylic acid can be increased when it is combined with Alectinib. Approved, Vet Approved Saquinavir The serum concentration of Saquinavir can be increased when it is combined with Alectinib. Approved, Investigational Selexipag The serum concentration of Selexipag can be increased when it is combined with Alectinib. Approved Silodosin The serum concentration of Silodosin can be increased when it is combined with Alectinib. Approved Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Alectinib. Approved Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Alectinib. Approved, Investigational Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Alectinib. Approved Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Alectinib. Approved, Investigational Sparfloxacin The serum concentration of Sparfloxacin can be increased when it is combined with Alectinib. Approved Sphingosine The serum concentration of Sphingosine can be increased when it is combined with Alectinib. Experimental Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Alectinib. Approved, Investigational Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Alectinib. Approved Taurocholic Acid The serum concentration of Taurocholic Acid can be increased when it is combined with Alectinib. Experimental Technetium Tc-99m sestamibi The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Alectinib. Approved Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Alectinib. Withdrawn Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Alectinib. Approved Ticagrelor The serum concentration of Ticagrelor can be increased when it is combined with Alectinib. Approved Timolol The serum concentration of Timolol can be increased when it is combined with Alectinib. Approved Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Alectinib. Approved Toremifene The serum concentration of Toremifene can be increased when it is combined with Alectinib. Approved, Investigational Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Alectinib. Approved Ulipristal The serum concentration of Ulipristal can be increased when it is combined with Alectinib. Approved Umeclidinium The serum concentration of Umeclidinium can be increased when it is combined with Alectinib. Approved Vecuronium The serum concentration of Vecuronium can be increased when it is combined with Alectinib. Approved Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Alectinib. Approved Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Alectinib. Approved Venlafaxine The serum concentration of Venlafaxine can be increased when it is combined with Alectinib. Approved Verapamil The serum concentration of Verapamil can be increased when it is combined with Alectinib. Approved Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Alectinib. Approved Vincristine The serum concentration of Vincristine can be increased when it is combined with Alectinib. Approved, Investigational Vismodegib The serum concentration of Vismodegib can be increased when it is combined with Alectinib. Approved Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Alectinib. Approved Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Alectinib. Approved - Food Interactions
- Not Available
References
- Synthesis Reference
- Not Available
- General References
- 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]
- 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]
- 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]
- 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
- KEGG Drug
- D10450
- PubChem Compound
- 49806720
- PubChem Substance
- 310265230
- ChemSpider
- 26326738
- BindingDB
- 50362781
- ChEBI
- 90936
- ChEMBL
- CHEMBL1738797
- PharmGKB
- PA166160050
- HET
- EMH
- RxList
- RxList Drug Page
- Wikipedia
- Alectinib
- ATC Codes
- Not Available
- AHFS Codes
- 10:00
- PDB Entries
- 3aox
- FDA label
- Download (581 KB)
- MSDS
- Not Available
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Capsule Oral 150 mg/1 Capsule Oral 150 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) US9126931 No 2011-05-29 2031-05-29 US US9440922 No 2010-06-09 2030-06-09 US US9365514 No 2012-03-04 2032-03-04 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source pKa 7.05 FDA Label - Predicted Properties
Property Value Source Water Solubility 0.0105 mg/mL ALOGPS logP 5.59 ALOGPS logP 4.89 ChemAxon logS -4.7 ALOGPS pKa (Strongest Acidic) 12.18 ChemAxon pKa (Strongest Basic) 6.97 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 72.36 Å2 ChemAxon Rotatable Bond Count 3 ChemAxon Refractivity 155.11 m3·mol-1 ChemAxon Polarizability 56.45 Å3 ChemAxon Number of Rings 6 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Carbazoles
- Direct Parent
- Carbazoles
- Alternative Parents
- Naphthalenes / Indoles / Aryl ketones / Dialkylarylamines / Aminopiperidines / Morpholines / Vinylogous amides / Heteroaromatic compounds / Pyrroles / Trialkylamines show 7 more
- Substituents
- Carbazole / Naphthalene / Indole / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Aryl ketone / 4-aminopiperidine / Morpholine / Oxazinane / Piperidine show 22 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not 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 a...
- 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 fro...
- 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 October 02, 2017 06:18