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Confirm mPDAC after prior therapy or when multiagent therapy is unsuitable
FDA-approved for metastatic pancreatic adenocarcinoma after ≥1 prior systemic therapy or when multiagent systemic therapy is not appropriate. The U.S. indication is not restricted by RAS mutation status and does not require a companion diagnostic.
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Baseline: CBC/CMP, Mg/Ca, LFTs, CA 19-9 + skin/oral/GI assessment
Before first dose: • CBC with differential and platelets.• CMP including sodium, potassium, creatinine/eGFR and glucose.• Liver profile: AST, ALT, ALP, total bilirubin and albumin.• Corrected calcium and magnesium.• CA 19-9. Interpret together with bilirubin and biliary obstruction/stent status.• Pregnancy test when applicable. Clinical baseline:• Weight and ECOG performance status.• Skin and oral examination.• Baseline bowel function, oral intake and hydration. If CA 19-9 is uninformative, consider CEA for disease monitoring.
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Before first dose: review CYP3A/P-gp and drug interactions adjust daraxonrasib if needed. Review concomitant medications
Avoid strong CYP3A inhibitors with P-gp inhibition and systemic cyclosporine A. Other strong/moderate CYP3A inhibitors and P-gp inhibitors require label-directed daraxonrasib dose adjustment. Avoid strong CYP3A inducers when possible; dose adjustment is required if unavoidable. Separate P-gp substrates from daraxonrasib by at least 4 hours. Do not use the adverse-reaction 300→200→150 mg dose ladder for drug interactions; interaction-specific doses are different.
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Before first dose: topical corticosteroid + emollient + SPF ≥30; consider doxycycline/minocycline
Start dermatologic prophylaxis before the first dose and continue during treatment as clinically appropriate: Apply a topical corticosteroid to the face and chest. Use emollient creams. Limit sun exposure. Use broad-spectrum sunscreen SPF ≥30. Consider prophylactic oral doxycycline or minocycline.
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Start daraxonrasib 300 mg once daily — with or without food; swallow tablets whole
Take daraxonrasib at the same time each day. Swallow tablets whole; do not chew, crush or split. If a dose is missed by >4 hours, skip it and take the next dose at the regularly scheduled time. If vomiting occurs after a dose, do not take an additional dose.
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First 8 weeks: repeat CBC/CMP/LFTs, Mg/Ca about q2 weeks; then q4 weeks if stable
Practical monitoring schedule: • Repeat CBC, renal/electrolyte profile, AST/ALT/ALP/bilirubin/albumin, corrected calcium and magnesium approximately every 2 weeks during the first 8 weeks. • If stable, repeat approximately every 4 weeks thereafter. • Check sooner for significant diarrhea, reduced oral intake, dehydration, new toxicity or prior laboratory abnormalities. • Repeat CA 19-9 with disease-response assessments; interpret trends rather than isolated values and do not use CA 19-9 as a substitute for imaging. The U.S. Prescribing Information does not mandate a fixed laboratory monitoring interval.
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New or worsening toxicity requiring intervention?
Assess CTCAE grade, symptom burden, oral intake/hydration, relevant laboratory abnormalities and serious red flags. Keep toxicity-specific grading within each branch rather than expanding the main flow.
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Yes
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Rash / dermatologic toxicity. 87% overall; Grade 3–4 13%
Assess extent, symptoms, skin integrity and impact on daily activities. Dermatologic toxicity may include rash, pruritus, paronychia, dry skin and skin fissures. Median time to first onset: 13 days.
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Topical corticosteroid ± doxycycline/minocycline; modify daraxonrasib by grade
Continue or intensify topical corticosteroid and emollient therapy. If not already receiving an oral antibiotic, consider doxycycline or minocycline as clinically appropriate. RASolute protocol prophylaxis used doxycycline 100 mg twice daily or minocycline 50 mg twice daily. Grade 2: • Consider withholding daraxonrasib until recovery to ≤Grade 1. • Resume at the same or next lower dose. Grade 3: • Withhold until recovery to ≤Grade 1. • Consider dermatology consultation. • Resume at the next lower dose. Grade 4: • Permanently discontinue daraxonrasib.
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Stomatitis / oral toxicity. 56% overall; Grade 3–4 12%
Assess grade and impact: mouth pain, mouth soreness, dysgeusia, oral mucositis, oral intake and hydration. Median time to first onset: 22 days.
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Stomatitis: start dexamethasone mouthwash; modify daraxonrasib by grade
Continue oral care. Supportive regimen: • Dexamethasone 0.5 mg/5 mL mouthwash: 10 mL TID; swish and spit. No food or drink for 30 minutes after use. • Clotrimazole lozenge 10 mg TID. Daraxonrasib modification: • Grade 2: consider withholding until recovery to ≤Grade 1; resume at the same or next lower dose. • Grade 3: withhold until recovery to ≤Grade 1; resume at the next lower dose. • Grade 4: permanently discontinue.
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Diarrhea. 67% overall; Grade 3–4 7%: assess hydration and oral intake
Diarrhea, nausea, vomiting, abdominal pain. Assess grade and impact. Assess stool frequency, duration, oral intake, hydration and clinically relevant electrolyte or renal abnormalities. Median time to first onset: 3 days.
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Start loperamide (4 mg initially, then 2 mg) + hydration; modify daraxonrasib by grade
Start antidiarrheal therapy promptly. Supportive regimen: • Loperamide 4 mg initially, then 2 mg after each loose stool; maximum 16 mg/day. • Maintain oral or IV hydration and replace electrolytes as clinically indicated. • Add antiemetics as needed. Daraxonrasib modification: • Grade 2 persistent or intolerable: consider withholding until recovery to ≤Grade 1; resume at the same or next lower dose. • Grade 3: withhold until recovery to ≤Grade 1; resume at the next lower dose. • Grade 4: permanently discontinue.
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Suspected ILD/pneumonitis or GI perforation. HOLD daraxonrasib and urgently evaluate
New or worsening dyspnea, cough or fever: • Withhold daraxonrasib and evaluate for ILD/pneumonitis. Severe or persistent abdominal pain or clinical concern for perforation: • Withhold daraxonrasib and urgently evaluate for gastrointestinal perforation. ILD/pneumonitis: • Grade 2: hold to ≤Grade 1; if appropriate, resume one dose lower. • Recurrent Grade 2 or Grade 3–4: permanently discontinue. GI perforation: • Grade 3: hold to ≤Grade 1; if appropriate, resume one dose lower. • Grade 4: permanently discontinue.
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Grade ≥3 laboratory or other clinically significant toxicity. Evaluate cause and severity
Evaluate relevant laboratory abnormalities and alternative/contributing causes, including disease-related factors, dehydration and concomitant medications. Grade according to CTCAE v5.0. Transaminase ↑, bilirubin ↑, cytopenias. Assess grade and trends.
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Other Grade 3 toxicity: hold to ≤G1/baseline + lower dose; Grade 4: discontinue
Grade 3: • Withhold daraxonrasib until recovery to ≤Grade 1 or baseline. • Resume at the next lower dose. Grade 4: • Permanently discontinue. Address reversible or competing causes before resumption when clinically appropriate.
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No
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Patient instructions: contact the care team early for rash, mouth sores, diarrhea, breathing symptoms or severe abdominal pain
Report promptly: • New or worsening rash, painful skin, blistering or extensive skin symptoms • Mouth sores or difficulty eating/drinking • Persistent or worsening diarrhea • New cough, dyspnea or fever • Severe or persistent abdominal pain
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How to take daraxonrasib: 300 mg once daily, with or without food; swallow tablets whole
Tablets are available as 100 mg and 150 mg. Take at the same time each day. Do not chew, crush or split tablets. Missed by >4 hours: skip the dose. Vomiting after a dose: do not repeat the dose.
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Dose Reduction Ladder
Starting dose: 300 mg once daily First reduction: 200 mg once daily (one 100 mg + one 100 mg) Second reduction: 150 mg once daily (one 150 mg) No further reduction below 150 mg Permanently discontinue if 150 mg once daily is not tolerated. Drug-interaction adjustments use a separate label-directed dosing scheme.
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Key drug interactions
Avoid strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, clarithromycin) → ↑ exposure Avoid strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St John’s wort) → ↓ exposure Avoid strong P-gp inhibitors (e.g., quinidine, cyclosporine) Avoid strong P-gp inducers (e.g., rifampin) Esomeprazole 40 mg daily: no clinically significant PK change
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Adverse reactions: frequency and severity
Rash: 87% | Grade 3–4: 13% Diarrhea: 67% | Grade 3–4: 7% Stomatitis: 56% | Grade 3–4: 12% Nausea: 52% | Grade 3–4: 3% Fatigue: 47% | Grade 3–4: 5% Vomiting: 42% | Grade 3–4: 1%
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Key red flags: hold and urgently evaluate
New or worsening dyspnea, cough, fever → evaluate for ILD/pneumonitis Severe or persistent abdominal pain → evaluate for GI perforation Any grade ≥3 or life-threatening AE
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Hepatic impairment: mild/moderate exposure unchanged; severe impairment not established
U.S. Prescribing Information: • Mild hepatic impairment: total bilirubin >ULN to 1.5×ULN, OR AST >ULN with normal bilirubin. • Moderate hepatic impairment: total bilirubin >1.5 to 3×ULN with any AST level. No clinically significant difference in daraxonrasib pharmacokinetics was observed with mild or moderate hepatic impairment. • Severe hepatic impairment: total bilirubin >3 to 10×ULN with any AST level. The effect of severe hepatic impairment on daraxonrasib pharmacokinetics is unknown.