Drug reference

Dabrafenib

BRAF kinase inhibitor (antineoplastic) · Antineoplastic

START

150 mg PO twice daily fasting (with trametinib)

TYPICAL MAX

300 mg/day

STOP IF

Serious febrile reaction, new malignancy, or severe haemorrhage

WATCH

Temperature/pyrexia, skin surveillance, glucose, ECG, eyes

CDSCO approvedSchedule HATC L01EC02

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · absorption
PEAK: 2h · Tmax
t½: 8h · t½
DURATION: 12h · twice-daily

EXCRETION

Mainly faecal; ~23% renal metabolites

route + CYP

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Can cause fetal harm — avoid; effective non-hormonal contraception (induces hormonal contraceptives).

FDA category + note

Top interactionssee all 12 →

Braf Wild Type TumourContraindicatedDatabaseKimi deep-research + Cla
Aminolevulinic AcidSevereDatabaseDDInter
AvapritinibSevereDatabaseDDInter
AvatrombopagSevereDatabaseDDInter

Mechanism

Selective ATP-competitive inhibitor of mutant BRAF V600 kinase, blocking constitutive MAPK pathway signalling; combined with a MEK inhibitor (trametinib) to delay resistance and reduce cutaneous toxicity.

Indications

BRAF V600-mutant melanoma (± trametinib)BRAF V600E NSCLC (with trametinib)BRAF V600E anaplastic thyroid cancer (with trametinib)BRAF V600E solid tumours (tissue-agnostic)

Dosing

Adult: 150 mg PO twice daily (≥1 h before or 2 h after meals), usually with trametinib 2 mg once daily.
Pediatric: Weight-based (paediatric LGG/solid tumours, with trametinib).
Renal adjustment: No adjustment for mild–moderate; not studied in severe.
Hepatic adjustment: Mild: no adjustment; moderate–severe: not studied — caution.
Geriatric: No specific adjustment.
Max dose: 300 mg/day (150 mg twice daily)

Pharmacokinetics

Onset

Tumour response over weeks

Peak effect

~2 h (Tmax)

Duration

~12 h (twice-daily)

Half-life

~8 h (active metabolites longer)

Bioavailability

~95% (reduced/variable with food)

Protein binding

~99.7%

Metabolism

Hepatic CYP2C8/CYP3A4 (active hydroxy/desmethyl metabolites)

Excretion

Mainly faecal; ~23% renal (metabolites)

Contraindications

BRAF wild-type tumours (paradoxical MAPK activation — possible tumour promotion)
Severe hypersensitivity
Caution: G6PD deficiency (haemolysis)

Side effects

Common

PyrexiaArthralgiaHyperkeratosisHeadacheFatigueNausea

Serious

Serious febrile reactions
Cutaneous squamous-cell carcinoma/new primary melanoma
Haemorrhage
Uveitis
QT prolongation
Hyperglycaemia
Severe pyrexia with hypotension/renal failure

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective non-hormonal contraception (induces hormonal contraceptives).

Lactation

Avoid breastfeeding during and 2 weeks after therapy.

Drug interactions

Braf Wild Type Tumour

Contraindicated

Database

Paradoxical MAPK activation

Confirm BRAF V600 mutation before use

Source: Kimi deep-research + Cla

Aminolevulinic Acid

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Avapritinib

Severe

Database