Colorectal Cancer Drug Summary

Last updated: 29 April 2025

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Cytotoxic Chemotherapy

Content on this page:

Cytotoxic Chemotherapy

Cytotoxic Chemotherapy



Drug Dosage Remarks
Capecitabine Metastatic CRC or as adjuvant treatment in stage III colon CA: 850-1,250 mg/m2 PO 12 hourly x 14 days
Repeat every 3 weeks
Combination treatment:
Initially, 1,000 mg/m2 PO 12 hourly for 2 weeks followed by a 7-day rest period
or
625 mg/m2 PO 12 hourly if administered continuously 		Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, stomatitis, abdominal pain, anorexia); Hematologic effects (neutropenia, leukopenia, thrombocytopenia, anemia); Dermatologic effects (hand-and-foot syndrome characterized by numbness, dysesthesia/paresthesia, tingling, swelling, erythema); Other effects (fatigue, headache)
Special Instructions
  • Doses should be taken with water within 30 minutes after a meal
  • Contraindicated in patients with severe hepatic and severe renal impairment (Cr <30 mL/min), in severe leukopenia, neutropenia or thrombocytopenia
  • Use with caution in patients with a history of significant cardiac disease, angina pectoris and arrhythmias, in patients with preexisting hyper- or hypocalcemia
  • Monitor intake in patients with mild-moderate liver dysfunction, regardless of the presence or absence of liver metastasis
Fluorouracil
(5-Fluorouracil, 5-FU)		 Initial dose:
Daily use: 15 mg/kg or 600 mg/m2as IV infusion over 2-4 hr/day
or
12 mg/kg or 480 mg/m2 slow IV (2-3 minutes) on day 1, 2 and 3 Weekly use:
15 mg/kg or 600 mg/m2 once weekly slow IV
or
5-7 mg/kg/day or 200 mg/m2/day as 24-hour IV infusion
Maintenance dose:
5-10 mg/kg IV or
200-400 mg/m2 IV once a week
Max dose: 1 g/day
Combination therapy with Leucovorin:
400 mg/m2 IV bolus on day 1, then 1,200 mg/m2 continuous IV infusion x 2 days every 2 weeks 		Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea); Hematologic effects (leukopenia, thrombocytopenia, neutropenia, anemia); CV effects (precordial pain and transient change in ECG)
Special Instructions
  • Contraindicated in patients with severe changes in blood count, bone marrow depression, hemorrhage, malabsorption, severe liver and renal impairment, severe infections, herpes zoster, varicella, stomatitis, ulcerations of the oral cavity and GIT, pseudomembranous enteritis, extensive liver metastasis
  • Use with caution in patients after high-dose pelvic irradiation, after therapy with alkylating substances and in severe bone metastasis
  • Avoid concomitant administration of live vaccine
  • Monitor blood count, liver and renal functions regularly
Ipilimumab Microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) metastatic CRC:
Combination treatment with Nivolumab:
1 mg/kg IV infusion over 30 minutes immediately following Nivolumab, administered on the same day every 3 weeks x 4 doses or until disease progression or intolerable toxicity 		Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain, decreased appetite); CNS effects (dizziness, headache); Respiratory effects (cough, dyspnea); Other effects (fatigue, rash, pyrexia, musculoskeletal pain, pruritus, arthralgia, hypothyroidism, decreased weight)
Special Instructions
  • Monitor for signs and symptoms of immune-mediated reactions including enterocolitis/colitis, hepatitis, dermatitis/adverse skin reactions, neuropathies, endocrinopathies (adrenal insufficiency, hyper- or hypothyroidism), pneumonitis, nephritis, encephalitis
Irinotecan Monotherapy for progressive/metastatic CRC:
Weekly (for 4 weeks followed by a 2-week rest period): 125 mg/m2 IV over 30-90 minutes
Once every 2 weeks: 180 mg/m2
Once every 3 weeks: 300-350 mg/m2 Doses to be given as IV infusion over 30-90 minutes
Combination therapy with Folinic acid (FA) and 5-FU in 1st-line metastatic CRC:
Regimen 1:
Irinotecan: 125 mg/m2 IV over 90 minutes
FA: 20 mg/m2 IV bolus injection
5-FU: 500 mg/m2 IV bolus injection
All doses to be taken on day 1, 8, 15 and 22 during a 6-week cycle; next cycle begins on day 43
Regimen 2:
Irinotecan: 180 mg/m2 IV over 30-90 minutes on day 1, 15 and 29
FA: 200 mg/m2 IV over 2 hours on day 1, 2, 15, 16, 29 and 30
5-FU bolus: 400 mg/m2 IV on day 1, 2, 15, 16, 29 and 30
5-FU infusion: (following bolus administration) 600 mg/m2 IV over 22 hours on day 1, 2, 15, 16, 29 and 30, during a 6-week cycle; next cycle begins on day 43
Combination therapy with FA and 5-FU (in previously untreated patients): Irinotecan: 180 mg/m2 once every 2 weeks followed by
FA: 200 mg/m2
Bolus 5-FU: 400 mg/m2
5-FU infusion: 600 mg/m2 IV infusion
Doses to be given as IV infusion over 30-90 minutes		 Adverse Reactions
  • GI effects (nausea/vomiting which can be severe, diarrhea which may become prolonged and severe >24 hours after a dose, abdominal pain, anorexia, constipation, mucositis, weight loss); Hematologic effects (neutropenia, leukopenia, thrombocytopenia); CNS effects (pain, dizziness, insomnia, headache); Other effects (fever, rash, malaise, reversible alopecia, weakness)
Special Instructions
  • Use with caution in patients with increased risk of diarrhea, those with previous abdominal/pelvic radiotherapy, those with renal or hepatic impairment; may impair ability to drive or operate machinery
  • Depending on patient’s ability to tolerate therapy, doses should be adjusted in increments of 25-50 mg/m2
  • Treatment should be delayed for 1-2 weeks to allow recovery from treatment-related toxicities. If patient has not recovered after the 2-week delay, consider discontinuing Irinotecan
  • Reduce initial/starting dose in patients with prior history of pelvic radiation or those with performance status of 2
  • Combination with FA and 5-FU: The dose of FA should be administered immediately after Irinotecan, with the 5-FU following immediately after
  • CBC should be monitored weekly during treatment
  • Liver function tests should be measured at baseline and prior to each cycle
Mitomycin Intermittent administration:
4-6 mg IV 24 hourly 1-2 times weekly
Continuous administration:
2 mg IV 24 hourly
Large-dose intermittent administration:
10-30 mg IV 24 hourly at 1-3 weeks intervals 		Adverse Reactions
  • GI effects (nausea/vomiting, gastritis, diarrhea, stomatitis, anorexia); Hematologic effects (thrombocytopenia, leukopenia, anemia, hemorrhage); Other effects (renal failure, hypertension, edema, hematuria, albuminuria, hemolytic-uremic syndrome, marrow depression, interstitial pneumonia)
Special Instructions
  • Avoid in patients with thrombocytopenia, coagulation disorder, or increased bleeding tendencies, hepatic failure, renal impairment and bone marrow suppression
  • Monitor patient frequently with lab tests; infectious disease, bleeding tendency
Oxaliplatin Monotherapy:
130 mg/m2 IV infusion over at least 2 hours every 3-4 weeks
Combination therapy with Oxaliplatin and Capecitabine:
130 mg/m2 IV every 3 weeks
Combination therapy with 5-FU with or without FA:
85 mg/m2 IV infusion over 2-6 hours every 2 weeks		 Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, mucositis, abdominal pain); Hematologic effects (anemia, neutropenia, thrombocytopenia, leukopenia, lymphopenia); CNS effect (acute, dose-cumulative peripheral sensory neuropathy); Other effects (fever, liver function abnormalities, alopecia, pharyngolaryngeal dysesthesia, infections)
Special Instructions
  • Contraindicated in patients with myelosuppression prior to starting first course, peripheral sensory neuropathy with functional impairment prior to first course, in severe renal impairment (CrCl <30 mL/min)
  • Use with caution in patients with moderately impaired renal function, history of allergic reaction to platinum compound
  • Perform neurological exam before each administration and periodically thereafter
  • Infusion rate should be reduced for patients who develop acute laryngopharyngeal dysesthesia
  • Perform CBC with WBC differential prior to start of treatment and before each subsequent course
  • Monitor renal function and for neurological toxicity
Tegafur1
(1-[2-tetrahydro-furyl]-5-FU)		 Combination therapy with FA:
Tegafur 300-600 mg/day + FA 75 mg/day PO in 3 divided doses
Repeat a course of a 28-day consecutive administration, followed by a 7-day rest period		 Adverse Reactions
  • Hepatic effects (severe hepatic disorder, hepatic cirrhosis); GI effects (severe diarrhea, severe enteritis, GI ulcer, severe stomatitis); Renal effects (acute renal failure, nephrotic syndrome); Hematologic effects (blood dyscrasias, hemorrhage); CV effects (angina pectoris, MI, arrhythmia); Other effects (severe psychoneurologic disorder, acute pancreatitis, interstitial pneumonia, anosmia, Stevens-Johnson syndrome)
Special Instructions
  • Should be taken on an empty stomach, 1 hour before or after meals
  • Avoid concomitant therapy with Sorivudine
  • Use with caution in patients with bone marrow depression, hepatic and renal impairment, infectious diseases, varicella, heart disease, glucose intolerance, GI ulcer or hemorrhage
  • Monitor hematologic, hepatic and renal function
Trifluridinetipiracil Initial dose:
35 mg/m2 PO 12 hourly within 1 hour after morning and evening meals on days 1-5 and days 8-12 of each 28-day cycle 
Max dose:
80 mg per dose
Continue treatment until disease progression or unacceptable toxicity 		Adverse Reactions
  • Hematologic effects (severe myelosuppression, anemia, neutropenia, thrombocytopenia); GI effects (nausea/vomiting, decreased appetite, diarrhea, abdominal pain, stomatitis); Other effects (asthenia/fatigue, pyrexia, alopecia, dysgeusia)
Special Instructions
  • Should be taken with food, within 1 hour after morning and evening meals
  • Obtain blood cell counts prior to and on day 15 of each cycle
  • Initiate treatment only when ANC is ≥1,500/mm3 or in the absence of febrile neutropenia, platelet count ≥75,000/mm3, grade 3 or 4 non-hematological adverse reactions are resolved to grade 0 or 1
  • Use with caution in patients with moderate-severe hepatic impairment and moderate renal impairment
1Combination with Gimeracil and Oteracil potassium is available. Please see the latest MIMS for specific formulations and prescribing information.

Other Antineoplastic Agent



Drug Dosage Remarks
Encorafenib Metastatic CRC with BRAF V600E mutation (in combination with Cetuximab):
300 mg PO 24 hourly
Continue until disease progression or unacceptable toxicity
Adverse Reactions
  • GI effects (nausea/vomiting, abdominal pain, decreased appetite); Dermatologic effects (rash, dermatitis acneiform); Other effects (fatigue, arthralgia)
Special Instructions
  • Detection of BRAF V600E mutational status must be done prior to initiation
  • Associated with moderate emetic potential; antiemetics may be given to prevent nausea/vomiting
  • Monitor electrolytes before and during treatment
  • Perform dermatologic evaluation prior to, while on therapy, and after discontinuation of treatment
  • Perform ophthalmologic evaluation at regular intervals

Supportive Care Therapy



Drug Dosage Remarks
Folinic acid
(Calcium folinate, Leucovorin) 		Advanced CRC (in combination with 5-FU)
Weekly regimen:
 20 mg/m2 IV bolus injection or
200-500 mg/m2 slow IV in a 2-hour infusion with 5-FU 500 mg/m2 as bolus injection
Bimonthly regimen:
200 mg/m2 slow IV infusion over 2 hours followed by 5-FU 400 mg/m2 IV bolus and 5-FU 600 mg/m2 22-hour IV infusion for 2 consecutive days every 2 weeks on days 1 and 2
Monthly regimen:
200 mg/m2 slow IV over at least 3 minutes (followed by 5-FU 370 mg/m2 IV)
or
20 mg/m2 IV (followed by 5-FU 425 mg/m2) Treatment is repeated daily for 5 days (each 5-day course may be repeated at 28-day intervals)
Advanced or metastatic CRC (in combination with Oxaliplatin and/or 5-FU)
400 mg/m2 IV on day 1 every 2 weeks
 Adverse Reactions
  • Hypersensitivity reactions have been reported; GI effects (nausea/vomiting, diarrhea)
Special Instructions
  • Contraindicated in patients with pernicious anemia or other megaloblastic anemia due to vitamin B12 deficiency
  • FA enhances toxicity of Fluorouracil; dose of FU may need to be adjusted
  • Obtain CBC with differential and platelet count prior to each treatment
  • Obtain electrolytes and liver function tests prior to each treatment for the first 3 cycles and then prior to every other cycle

Targeted Cancer Therapy



Drug Dosage Remarks
Monoclonal Antibodies
Bevacizumab Metastatic CRC as 1st-line treatment (as IV infusion):
5 mg/kg body wt once every 2 weeks
or
7.5 mg/kg body wt once every 3 weeks
Metastatic CRC as 2nd-line treatment (as IV infusion):
10 mg/kg body wt once every 2 weeks
or
15 mg/kg body wt once every 3 weeks
Continue treatment until disease progression or unacceptable toxicity 		Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, abdominal pain, intestinal perforation, ileus, intestinal obstruction, anorexia, stomatitis); Hematologic effects (leukopenia, thrombocytopenia, neutropenia, anemia, febrile neutropenia, lymphopenia); CV effects (hypertension, arterial and venous thromboembolism, cardiac failure); Other effects (headache, asthenia, fatigue, necrosis, post-op bleeding or wound healing complications, proteinuria, tumor-associated bleeding, eye disorders, peripheral sensory neuropathy, sepsis, abscess, cellulitis, infections, dehydration, hyponatremia)
Special Instructions
  • Should not be administered as IV bolus or push
  • Contraindicated in untreated CNS metastases, in patients with recent pulmonary hemorrhage/hemoptysis
  • Use with caution in patients with hypertension, hemorrhage, neutropenia, wound healing complications, proteinuria, arterial thromboembolism, cardiomyopathy, congestive heart failure, reversible posterior leukoencephalopathy, renal and hepatic impairment
  • Discontinue permanently if GI perforation develops, in patients who experience grade 3 or 4 bleeding during therapy, if medically significant hypertension cannot be adequately controlled with antihypertensive therapy or if the patient develops hypertensive crisis or hypertensive encephalopathy
  • BP monitoring while on therapy is recommended
  • Therapy should not be initiated for at least 28 days following a major surgery or until the surgical wound is fully healed
Cetuximab Initial dose:
400 mg/m2 IV infusion over 2 hours on first week
or
500 mg/m2 IV infusion over 2 hours on day 1 every 2 weeks Maintenance dose:
250 mg/m2 IV infusion over 1 hour weekly
Max infusion rate:
10 mg/min

Adverse Reactions

  • Mild to moderate infusion-related reactions (chills, fever, dizziness, dyspnea) may occur; Severe infusion-related reactions (bronchospasm, urticaria, hypotension, loss of consciousness or shock) usually occur within 1 hour of first infusion
  • GI effects (mild-moderate mucositis, nausea/vomiting, diarrhea, anorexia, increased liver enzyme levels); Metabolic effects (hypomagnesemia, hypocalcemia); Other effects (headache, conjunctivitis)

Special Instructions

  • Detection of KRAS mutational status must be done before initiating Cetuximab
  • Prior to infusion, premedicate with an antihistamine and a corticosteroid
  • Concomitant chemotherapeutic agents must not be administered earlier than 1 hour after Cetuximab infusion
  • Contraindicated in known severe (grade 3 or 4) hypersensitivity reactions to Cetuximab
  • Monitor for infusion-related reactions
  • Monitor serum electrolyte levels
Dostarlimab
 MSI-H/dMMR or POLE/POLD1 mutation-positive metastatic CRC
500 mg IV infusion over 30 minutes every 3 weeks x 4 cycles followed by 1,000 mg IV every 6 weeks until disease progression or unacceptable toxicity

Adverse Reactions

  • GI effects (nausea/vomiting, diarrhea, colitis, pancreatitis); Hematologic effects (anemia, decreased lymphocytes); Metabolic effects (decreased sodium, increased alkaline phosphatase, decreased albumin, increased transaminases, hypothyroidism); Musculoskeletal effects (arthralgia, myalgia); Other effects (pneumonitis, fatigue, asthenia, rash, pruritus, pyrexia, chills)

Special Instructions

  • Use with caution in patients with history of allogeneic hematopoietic stem cell transplantation (HSCT)
  • Monitor for signs and symptoms of immune-mediated adverse reactions (pneumonitis, colitis, hepatitis, endocrinopathies, nephritis, rash, arthralgia)
  • Evaluate clinical chemistries, including liver enzymes, creatinine, and thyroid function at baseline and periodically during treatment
Fam-trastuzumab deruxtecan-nxki 5.4 mg/kg IV on day 1
Cycled every 21 days

Adverse Reactions

  • GI effects (nausea/vomiting, constipation, diarrhea); Hematologic effects (neutropenia, leukopenia, thrombocytopenia, anemia); Other effects (decreased appetite, cough, alopecia, fatigue)

Special Instructions

  • Use with caution in patients at risk for severe, life-threatening, or fatal interstitial lung disease (ILD), severe neutropenia including febrile neutropenia, cardiac disorders
  • Monitor CBC and assess LVEF prior to initiation and prior to each dose, and as clinically indicated
Nivolumab MSI-H/dMMR or POLE/POLD1 mutation-positive metastatic CRC
Monotherapy:
3 mg/kg IV infusion over 30 minutes 2 weekly or 240 mg IV infusion over 60 minutes every 2 weeks or 480 mg IV infusion over 30 minutes every 4 weeks
Continue treatment until disease progression or unacceptable toxicity
Combination therapy with Ipilimumab: 3 mg/kg IV infusion over 30 minutes once every 3 weeks x 4 doses

Adverse Reactions

  • Dermatologic effects (Stevens-Johnson syndrome, toxic epidermal necrolysis, rash, pruritus); Metabolic effects (adrenal insufficiency, type 1 DM, diabetic ketoacidosis); GI effects (diarrhea/colitis, nausea/vomiting, constipation, abdominal pain, intestinal perforation, stomatitis); Hematologic effects (neutropenia, lymphocytopenia, anemia, leukopenia, thrombocytopenia); Hepatic effects (hepatitis; elevation of ALT, AST, alkaline phosphatase, bilirubin); Respiratory effects (pneumonia, pneumonitis or interstitial lung disease, pulmonary embolism, dyspnea); CV effect (hypertension); Renal effects (renal failure, immune-mediated nephritis); Other effects (hypophysitis, increased serum amylase, lipase, cholesterol; hyponatremia, immune-mediated encephalitis, thyroid dysfunction)

Special Instructions

  • Use with caution in cases of moderate to severe hepatic impairment
  • Monitor liver function tests, serum creatinine, thyroid function at baseline, blood glucose
  • Monitor for signs and symptoms of electrolyte imbalance
Panitumumab Monotherapy and in combination with FOLFOX or FOLFIRI:
6 mg/kg IV infusion over 60 minutes every 2 weeks (90 minutes for doses >1,000 mg)

Adverse Reactions

  • Dermatologic effects (acneiform rash, dermatitis, pruritus, erythema, paronychia); Mild to moderate infusion-related reactions (chills, fever, dizziness, dyspnea) may occur; Severe infusion-related reactions (bronchospasm, urticaria, hypotension, loss of consciousness or shock) usually occur within 1 hour of first infusion; GI effects (diarrhea may occur and severity is increased with combination therapy, abdominal pain, nausea/vomiting, constipation, stomatitis); Other effects (cough, fatigue, magnesemia, hypocalcemia)

Special Instructions

  • Detection of wild-type RAS (KRAS and NRAS) status is required before initiating treatment
  • Do not administer as intravenous push or bolus
  • Contraindicated in patients with life-threatening reactions to Panitumumab, in those with mutant RAS metastatic colorectal CA or for whom RAS status is unknown
  • Use with caution in dermatologic reactions and soft tissue toxicity, infusion-related reactions, pulmonary complications, electrolyte disturbances, renal or hepatic impairment
  • Reduce infusion rate by 50% in mild-moderate (grade 1 or 2) infusion reactions; discontinue use immediately and permanently should a severe (grade 3 or 4) infusion reaction occur
  • Discontinue use if severe dermatological toxicity develops
  • Monitor serum electrolytes
Pembrolizumab Metastatic dMMR/MSI-H or POLE/POLD1 mutation-positive:
2 mg/kg IV 3 weekly or 200 mg IV infusion over 30 minutes 3 weekly or 400 mg IV infusion over 30 minutes 6 weekly Continue treatment until disease progression or unacceptable toxicity
Max duration: 2 years

Adverse Reactions

  • Immune-mediated reactions (colitis, DM, hepatitis, hypothyroidism or hyperthyroidism, hypophysitis, nephritis, pneumonitis); Other effects (diarrhea, pyrexia, arthralgia, back pain, cough, vitiligo, abdominal pain, rash, pruritus, hyponatremia)

Special Instructions

  • Use with caution in patients with autoimmune disorders, recipient of allogeneic HSCT or solid organ transplant
  • Monitor for signs and symptoms of immune-mediated adverse reactions such as pneumonitis, colitis, hepatitis, endocrinopathies, nephritis
  • Withhold use if with moderate grade 2 pneumonitis, grade 2-3 colitis, grade 2 nephritis or hypophysitis, AST/ALT >3 to 5x ULN or total bilirubin >1.5 to 3x ULN; discontinue permanently if with grade 3-4 pneumonitis, grade 4 colitis, grade 3-4 nephritis or hypophysitis, AST/ALT >5x ULN or total bilirubin >3x ULN
Ramucirumab Combination therapy with Irinotecan, FA and 5-FU (FOLFIRI):
8 mg/kg given as an IV infusion over 60 minutes once every 2 weeks prior to FOLFIRI
Continue treatment until disease progression or unacceptable toxicity occurs

Adverse Reactions

  • Hematologic effects (neutropenia, thrombocytopenia leukopenia); GI effects (GI hemorrhage, stomatitis, diarrhea, abdominal pain); CV effect (hypertension); Other effects (asthenia, fatigue, proteinuria, peripheral edema, palmar-plantar erythrodysesthesia, mucosal inflammation, epistaxis, hypoalbuminemia)

Special Instructions

  • Premedication with H1-receptor antagonist (eg Diphenhydramine) prior to infusion is recommended
  • Discontinue use with GI perforation, fistula formation, grade 3 or 4 bleeding, severe arterial thromboembolic events, urine protein level >3 g/24 hr, significant hypertension not controlled with antihypertensive therapy
  • Reduce dose by 50% for the duration of the infusion and all subsequent infusions if patient experiences grade 1 or 2 infusion-related reactions; permanently discontinue in the event of grade 3 or 4 infusion-related reactions
  • Use with caution in cases of hypertension, severe liver cirrhosis, severe renal impairment
  • Monitor blood counts and coagulation parameters
  • Monitor BP prior to each administration
  • Should be temporarily suspended for at least 4 weeks prior to elective surgery
Trastuzumab Combination therapy with Pertuzumab:
8 mg/kg IV loading dose on day 1 of cycle 1, followed by 6 mg/kg IV every 21 days 
Combination therapy with Lapatinib:
4 mg/kg IV loading dose on day 1 of cycle 1, followed by 2 mg/kg IV weekly
Combination therapy with Tucatinib:
8 mg/kg IV loading dose on day 1 of cycle 1, followed by 6 mg/kg IV every 21 days  

Adverse Reactions

  • CNS effects (headache, dizziness, insomnia, peripheral neuritis); Dermatologic effects (acne, rash, severe hypersensitivity reaction eg anaphylaxis); GI effects (abdominal pain, anorexia, diarrhea, nausea/vomiting); CV effects (edema, palpitation, hypotension, heart failure); Hematologic effects (leukopenia, anemia); Other effects (infusion-related symptoms [eg fever, chills]; rash, weakness, back pain, dyspnea, cough)

Special Instructions

  • Use with caution in patients with preexisting cardiac disease, previous exposure to radiation therapy or anthracyclines
  • Monitor cardiac function at baseline, during and after treatment
 Other Antineoplastic Agent
 Adagrasib KRAS G12C mutation (in combination with Cetuximab):
600 mg PO 12 hourly Treatment is continued until disease progression or unacceptable toxicity occurs

Adverse Reactions

  • CV effects (edema, prolonged QT interval); Endocrine/metabolic effects (decreased serum albumin, decreased serum magnesium & potassium); GI effects (nausea/vomiting, diarrhea, abdominal pain, decreased appetite); Hematologic effects (decreased platelet count, lymphocytopenia); Hepatic effects (increased ALT and AST); CNS effects (fatigue, nervousness); Respiratory effects (cough, dyspnea, pneumonia); Other effects (increased creatinine, musculoskeletal pain)

Special Instructions

  • Antiemetics may be taken to prevent nausea/vomiting
  • Avoid use in patients with congenital long QT syndrome and those with concurrent QTc prolongation and in patients taking other medications known to prolong QTc interval
  • Monitor LFTs, ECG and electrolytes prior to treatment initiation and as clinically indicated
Protein Kinase Inhibitors
Entrectinib NTRK gene fusion-positive:
600 mg PO 24 hourly

Adverse Reactions

  • GI effects (constipation, dysgeusia, diarrhea, nausea/vomiting); CNS effects (dizziness, cognitive impairment); Respiratory effects (dyspnea, cough); Musculoskeletal effects (myalgia, arthralgia); Other effects (fatigue, edema, dysesthesia, increased weight, pyrexia, vision disorders)

Special Instructions

  • Use with caution in patients with new or worsening CHF, myocarditis, QT prolongation, at risk for fractures, hyperuricemia
  • Assess LVEF, serum uric acid levels prior to initiation of therapy
  • Monitor liver tests, including ALT and AST, every 2 weeks during the first month of treatment, then monthly thereafter, and as clinically indicated
  • Withhold treatment for new-onset or worsening CHF, new visual changes or changes that interfere with activities of daily living or presence of CNS effects (cognitive impairment, mood disorders, dizziness, sleep disturbances)
Fruquintinib 5 mg PO 24 hourly for the first 21 days of each 28-day cycle Treatment is continued until disease progression or unacceptable toxicity occurs 

Adverse Reactions

  • Hematologic effects (decreased platelet count, hemorrhage); GI effects (diarrhea, abdominal pain or discomfort, decreased appetite); Other effects (hypertension, hand-foot skin reaction, proteinuria, abnormal hepatic function, increased blood bilirubin, fatigue, asthenia)

Special Instructions

  • Swallow capsules whole with water
  • Contraindicated in patients with severe active hemorrhage, active GI ulcer, unhealed GI perforation or fistula, severe hepatic or renal impairment
  • Routine monitoring of CBC, coagulation indicators, LFTs at baseline and during treatment and monitor BP once a week in the first 3 cycles and once per cycle thereafter
Larotrectinib NTRK gene fusion-positive:
100 mg PO 12 hourly

Adverse Reactions

  • GI effects (nausea/vomiting, constipation, diarrhea); CNS effects (delirium, gait disturbance, dysarthria, dizziness, paresthesia, memory impairment); Other effects (increased AST/ALT, anemia, fatigue, cough)

Special Instructions

  • Swallow capsules whole with water
  • Use with caution in patients with hepatic impairment, women of childbearing potential
  • Withhold or permanently discontinue if with neurologic adverse reactions
Regorafenib Metastatic CRC:
160 mg PO 24 hourly for the first 21 days of each 28-day cycle 
or
1st cycle:
80 mg PO 24 hourly on days 1-7 followed by 120 mg PO 24 hourly on days 8-14, followed by 160 mg PO 24 hourly on days 15-21
Subsequent cycles:
160 mg PO 24 hourly on days 1-21
Repeat every 28 days

Adverse Reactions

  • GI effects (decreased appetite, diarrhea, mucositis, hepatotoxicity, GI perforation); CV effect (hypertension); Other effects (asthenia, fatigue, weight loss, dysphonia, hand-foot skin reaction, infection, hemorrhage, pain)

Special Instructions

  • Should be taken with food at the same time each day with a low-fat meal
  • Discontinue use with GI perforation or fistula, wound dehiscence
  • Not recommended in patients with severe hepatic impairment
  • Use with caution in cases of hemorrhage, hepatotoxicity, unstable or new onset angina, recent MI, ischemia, cardiac failure NYHA class 2, hypertension
  • Obtain liver function tests (ALT, AST, bilirubin) before initiating therapy and closely monitor (at least every 2 weeks) during the first 2 months of treatment, then continue periodic monitoring at least monthly thereafter and as clinically indicated
  • Monitor blood counts and coagulation parameters in patients predisposed to bleeding or taking anticoagulants
  • Monitor biochemical and metabolic parameters during treatment
Selpercatinib RET gene fusion-positive:
<50 kg: 120 mg PO 12 hourly
≥50 kg: 160 mg PO 12 hourly  

Adverse Reactions

  • GI effects (dry mouth, diarrhea, constipation); Metabolic effects (increased AST/ALT, increased glucose, increased creatinine, increased alkaline phosphatase, increased total cholesterol, decreased albumin, decreased calcium, decreased sodium); Hematologic effects (decreased leukocytes, decreased platelets); Other effects (hypertension, fatigue, edema, rash)

Special Instructions

  • Use with caution in patients with significant risk of developing QTc prolongation
  • Contraindicated in patients with uncontrolled hypertension
  • Monitor AST/ALT prior to initiation of therapy, every 2 weeks during the first 3 months, then monthly; monitor BP 1 week after treatment initiation, then at least monthly thereafter
Tucatinib RAS wild-type HER2-positive unresectable or metastatic CRC in combination with Trastuzumab:
300 mg PO 12 hourly Treatment is continued until disease progression or unacceptable toxicity occurs

Adverse Reactions

  • GI effects (nausea/vomiting, diarrhea, abdominal pain, stomatitis, decreased appetite); Hematologic effect (anemia); Dermatologic effects (palmar-plantar erythrodysesthesia, rash); Other effects (hepatotoxicity, fatigue, headache)

Special Instructions

  • Use with caution in patients with new or worsening respiratory symptoms, hepatic impairment, venous thromboembolism
  • Monitor ALT, AST and bilirubin prior to initiation, every 3 weeks and as clinically indicated
Ziv-aflibercept
(Aflibercept)		 Metastatic CRC (in combination with FOLFIRI) resistant to or has progressed after an Oxaliplatin-containing regimen:
 4 mg/kg IV infusion over 1 hour
Treatment is continued until disease progression or unacceptable toxicity occurs  

Adverse Reactions

  • Hematologic effects (leukopenia, neutropenia, thrombocytopenia); GI effects (diarrhea, abdominal pain, decreased appetite, stomatitis); Hepatic effects (elevated AST, ALT levels); Other effects (elevated serum creatinine, fatigue, epistaxis, hypertension, weight loss, dysphonia, headache)

Special Instructions

  • Administered only as an IV infusion over 1 hour
  • Use with caution in patients with severe renal impairment (due to very limited data in these patients)
  • Discontinue use in cases of severe hemorrhage, GI perforation, fistula formation, inadequately controlled hypertension, cardiac failure and decreased ejection fraction, in hypertensive crisis or hypertensive encephalopathy, arterial thromboembolic events, grade 4 VTE (including pulmonary embolism), nephrotic syndrome or thrombotic microangiopathy, severe hypersensitivity reactions (including bronchospasm, angioedema and anaphylaxis), compromised wound healing requiring medical intervention, reversible posterior leukoencephalopathy syndrome
  • Should be temporarily suspended for at least 4 weeks prior to elective surgery
  • Monitor CBC with platelet and differential counts prior to each cycle


Disclaimer

All dosage recommendations are for non-pregnant and non-breastfeeding women and non-elderly adults with normal renal and hepatic function unless otherwise stated. 
Not all products are available or approved for above use in all countries. 
Products listed in the Drug Summary are based on indications stated in the locally approved product monographs. 
Please refer to local product monographs in Related MIMS Drugs for country-specific prescribing information.  

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