• Refer to your local label for recommended administration methods for Alecensa.
• Alecensa is formulated as an immediate-release, hard, size 1 capsule. There are currently no commercially available suspensions of alectinib chloride.
• Alecensa capsules should be taken with food and swallowed whole.
• A Phase 1 crossover, open-label, randomised study evaluated the relative bioavailability and pharmacokinetics (PK) of an Alecensa suspension versus capsule formulation in 28 healthy adult subjects:
• The oral Alecensa suspension showed significantly higher peak and overall exposure than the Alecensa capsules, under fed and fasted conditions in healthy adults.
• There were no apparent differences in incidence or severity of treatment-emergent adverse events between formulations.
• Clinical experience of preparing suspensions from Alecensa capsules for administration in the setting of non-small cell lung cancer (NSCLC) is limited to case reports in patients fitted with feeding tubes.

AE= Adverse event

CT= Computerised tomography

NG= Nasogastric

NSCLC= Non Small Cell Lung Cancer

PEG= Percutaneous Endoscopic Gastrotomy 

PET= Positron emission tomography

PK= Pharmacokinetics

Alecensa capsules should be taken with food and swallowed whole. Do not open or dissolve the contents of the capsule.[1] Refer to the local label for Alecensa administration and handling information.

There are currently no commercially available solutions of alectinib hydrochloride. Data on efficacy has not been established with alternative dosage forms and routes of administration.

The decision whether to open Alecensa capsules lies with the physician and should be based on an appropriate assessment of the likely risk:benefit ratio. If Alecensa capsules were opened to make a suspension or sprinkle over food, we would advise appropriate clinical caution and monitoring.

Alecensa is formulated as an immediate-release, hard, size 1 capsule. The contents of an Alecensa capsule is white to yellow white powder, or powder with lumps.

Be aware that

• Alecensa is categorised as an anti-neoplastic agent,
• Alecensa has low solubility in aqueous buffers across the entire pH range, [2]
• opening capsules may scatter its ingredients, leading to inhalation and contact with active ingredients, and
• food compatibility studies have not been undertaken, therefore stability or drug release properties cannot be determined if the capsule contents are sprinkled on food.

Caution is advised if capsules are opened. 

The relative bioavailability and pharmacokinetics of Alecensa administered as an oral suspension versus capsule was assessed in healthy adults under fasted and fed conditions.[3] This Phase I, crossover, open-label, randomised study was performed to infer suitability of Alecensa administered as a suspension to paediatric patients who cannot swallow capsules.

28 healthy adult volunteers received two single-dose Alecensa doses, two weeks apart. Volunteers were fed or fasted and were given doses of

• 4 x 150 mg Alecensa capsules (600mg total) and
• 600 mg Alecensa oral suspension.

The oral suspension was prepared by adding the contents of four 150 mg Alecensa capsules to 20 mL water to yield a drug concentration suspension of 30 mg/mL. This suspension was gently mixed (1:1) with apple juice and ingested within two hours of preparation.

The combined alectinib and M4 (active metabolite) exposure was higher for the suspension versus the capsules. The presence of food increased alectinib exposure regardless of formulation. Table 1 provides the relative bioavailability of alectinib and M4.

Table 1. Primary PK endpoints

Abbreviations: AUC0-∞= area under the concentration–time curve extrapolated to infinity; AUC0-t= area under the concentration–time curve from time 0 to the last measurable concentration; CI= confidence interval; Cmax= maximum observed concentration; GMR= geometric mean ratio; PK= pharmacokinetic.

Single doses of 600mg alectinib oral suspension and capsules were well tolerated, with no serious AEs, AEs of special interest, or grade ≥3 AEs reported. 

There were no observed differences in the incidence or severity of treatment-emergent AEs between formulations. Treatment-related AEs were reported in three subjects (10.7%) and included somnolence, abdominal pain, and headache; all were grade 1 in severity and were resolved at study completion. 

Study summary

Alecensa suspension showed significantly higher peak and overall exposure than the Alecensa capsules under fed and fasted conditions in healthy adults. Poor solubility of alectinib is likely to have cause this effect. The publication authors stated that generating an oral suspension by vigorous stirring of capsule contents may have increased the soluble fraction, leading to increased drug absorption compared to intact capsules. The study concluded that an oral Alecensa suspension may be suitable for paediatric studies after appropriate dose adjustment. 

The full publication provides more information on the PK and potential dose adjustment requirements.[3]

Case reports of patients receiving an Alecensa suspension have been published. Table 2 describes these case reports in more detail. All patients in the case reports had stage IV ALK-NSCLC.

Table 2. Case reports of patients receiving Alecensa by suspension

Abbreivations: BD = Twice a day, CR=complete response, OD = Once a day, 1L = First line, 2L = Second line

1. Roche Internal Regulatory Document (Accessed July 2023).
2. Center for Drug Evaluation and Research: application number 208434Orig1s000, chemistry review(s): 4-7. Hoffmann-La Roche Inc. 2015;https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208434Orig1s000ClinPharmR.pdf
3. Liu S, Agarwal P, Heinig K, et al. Relative bioavailability and food effect study of an oral suspension of alectinib in healthy volunteers using venipuncture and capillary microsampling. Clin Transl Sci 2023;16:1085-1096. https://www.ncbi.nlm.nih.gov/pubmed/36978270
4. Watanabe Y, KN, IY, et al. Successful alectinib treatment for a mechanically ventilated patient with ALK-positive non-small cell lung cancer. Ann. Cancer Res. Ther 2016;24:47-51. https://www.jstage.jst.go.jp/article/acrt/24/2/24_47/_pdf
5. Kanai O, Kim Y, Nakatani K, et al. Nasogastric tube-administered alectinib achieved long-term survival in a crizotinib-refractory nonsmall cell lung cancer patient with a poor performance status. Clin Case Rep 2017;5:927-930. https://www.ncbi.nlm.nih.gov/pubmed/28588841
6. Bejarano VM, Gould S, Charlot M. Response to alectinib oil-based suspension in anaplastic lymphoma kinase-positive non-small cell lung cancer in a patient unable to swallow: A case report. J Oncol Pharm Pract 2019;25:1722-1725. https://www.ncbi.nlm.nih.gov/pubmed/30124125
7. Anderson B, Luczak T, Ries L, et al. Successful alectinib desensitization in a patient with anaplastic lymphoma kinase-positive adenocarcinoma of the lung and alectinib-induced drug rash. J Oncol Pharm Pract 2020;26:2028-2030. https://www.ncbi.nlm.nih.gov/pubmed/32476587
8. Thomas Q, Pautas M, Guilhaume M, et al. Enteral administration of alectinib for ALK-positive non-small cell lung cancer in an elderly patient: A case report. Medicine (Baltimore) 2021;100:e27611. https://www.ncbi.nlm.nih.gov/pubmed/34713842
9. Ishiura Y, Nomura S, Ishii Y, et al. Alectinib in a patient with ALK-positive non-small lung cancer unable to swallow capsules. J Oncol Pharm Pract 2023;10781552231155374. https://www.ncbi.nlm.nih.gov/pubmed/36740945