Drug General Information
Drug ID D00FGR
Drug Name Miltefosine
Synonyms HDPC; HePC; Hexadecylphosphocholine; Hexadecylphosphorylcholine; Impavido; Miltefosina; Miltefosinum; Miltex; Baxter Oncology brand of miltefosine; Baxter brand of miltefosine; Miltefosin C; Prasfarma brand of miltefosine; D 18506; IN1227; D-18506; H-1850; M-7200; Miltefosina [INN-Spanish]; Miltefosine (INN); Miltefosine[INN:BAN]; Miltefosinum [INN-Latin]; N-Hexadecylphosphorylcholine; TF-002; Choline hydroxide, hexadecyl hydrogen phosphate, inner salt; Choline, hexadecyl hydrogen phosphate, inner salt; Hexadecyl 2-(trimethylazaniumyl)ethyl phosphate; Choline phosphate, hexadecyl ester, hydroxide, inner salt; Choline phosphate, hexadecyl ester, hydroxide, inner salt (6CI); Hexadecyl 2-(trimethyl-.lambda.~5~-azanyl)ethyl hydrogen phosphate; Ethanaminium, 2-(((hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethyl-, hydroxide, inner salt; Ethanaminium, 2-(((hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethyl-, hydroxide, innner salt; 1-Hexadecylphosphorylcholine; 2-(((Hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethylethanaminium hydroxide, inner salt; 3,5-Dioxa-4-phosphaunacosan-1-aminium, 4-hydroxy-N,N,N-trimethyl-, hydroxide, inner salt, 4-oxide
Drug Type Small molecular drug
Therapeutic Class Antifungal Agents
Company Aeterna Zentaris
Structure D00FGR
Drug Resistance Mutations
Target Name Parasitic Phospholipid-transporting ATPase (LdMT) Target Info
Gene Name LdMT
Uniprot ID Q6VXY9_LEIDO
Species Leishmania donovani
Reference Sequence MPNQPPCWRKCLSTRIFPDKLSKSFCCFSAEADVDEDDEVIVYLNDPELNAQFNYPSNFI
RTSKYTLISFLPLSLLLEFKKVSNLYFLMNVIFSLIPGVSPLSPATSIAPLSFVLIVALI
KEGVEDIKRHQADNRANSILVQVLRNGKLVSVHSKDIHPGDVMRIKNGEEVRADVVMLAS
SVEEGQAFIDTCNLDGETNLKSRKALEATWALCEVEAIMNSTAVLHTSKPDPGLLSWAGL
LEINGEEHALSLNQFLYRGCVLRNTDWVWGMVAYAGVDTKLFRNLKPKPPKSSNLDRKLN
YFIIAILIFQNIMLFILASMAVWWNSKYRETPYLRFFISFRKNVTLWGYRYLSYFILLSY
CVPISLFITIEVCKVVQAQWMRVDCLMMEYMSNRWRHCQPNTSNLNEQLAMVRFIFSDKT
GTLTENVMKFKLGDALGNPIDADNLDECIAQLRKEAESKGLGPLQEYFLALALCNTVQPF
KDDTDDLGVVYEGSSPDEVALVETAAAVGYRLISRTTKSITLLLHDGTRKVYNILATLEF
TPDRKMMSIIVEDSDTKKITLYNKGADSFIRPQLSRAPDVQGHIENVEIPLTEMSSSGLR
TLLVCAKDITRRQFDPWFEKFVEAGKSLHNRSSNIDKVCLEMEQDMRLVGATAIEDKLQD
EVPETLSFFLSAGVIIWMLTGDKRETAVTIAATSTLCDPRNDFIDHIDIGHLNSSDPKAI
ERVGRDLEVVEQHIALKGTHKERRCTLVIDGPALNIAMEHYFDQFLRLSHQVNSAVCCRL
TPIQKATVVRMFQKSTGKTALAIGDGANDVSMIREGRVGVGIIGLEGAHAALAADYAIPR
FKHLRRLCAVHGRYSLFRNASCILVSFHKNITVSVVQFIFAFYVGFSGLTLFDGWMLTFY
NVLLTSIPPFFMGIFDKDLPEDALLERPKLYTPLSHGEYFNLATLLRWFVESLTTAVILF
YAAYPTLIRQDGSHQRYTGGETGTLVFSGLILVIQTRFILQIRYWQWLQVFGMAMSIFLF
LLLFLVYSAIPSVFSDTNFYYQAFDLMSTAKYWFFLLLYVGTEVVVVLGVMTFQKNLFPT
LRDVAERQYAVQNGGKL [Leishmania donovani]
Targeted Disease Leishmaniasis
Drug Resistance Mutations
Mutation info Missense: M381T [1], [2]
Mutation info Missense: F1078Y [2]
Target Name Parasitic Phospholipid-transporting ATPase (Ros3) Target Info
Gene Name Ros3
Uniprot ID Q0P0L8_LEIDO
Species Leishmania donovani
Reference Sequence MAPLPPKPHSKNRIEQQQLPHIYARHSPLSVSVVFFILAVAAIPIGVLVIVSGDLTTRLD
FRYDHINSYKFAMGAAGEFAVNFPFNGTMYSSGVKTRLMFSLHQSLTAPVYMQYRLSPFF
QNYRYFTASVDYSQLSGRASAISKLCAPFRFPGEATGDSVSGYYNPCGAYPWAMFNDSIS
LYRTDGTLICDGSAFTANGTSLAANNKCVKSGIARPSDVKERYNPPREIPGNGPMWSAGG
NKSATDPYLREGYYYKEPGHKIPLSIDEDLIVWLDPAFTSDVTKNYRILNVDLPAGDYYF
EITEQYPTAPYASHKFVQLATRSWIGGRSHVLGSLLIIMGGTAFIMAVTLLSVKYLIMPV
YTEDI [Leishmania donovani]
Targeted Disease Leishmaniasis
Drug Resistance Mutations
Mutation info Missense: Y354F [2]
Target Name Fungal Metacaspase-1 (MCA1) Target Info
Gene Name MCA1
Uniprot ID MCA1_YEAST
Species Saccharomyces cerevisiae
Reference Sequence MYPGSGRYTYNNAGGNNGYQRPMAPPPNQQYGQQYGQQYEQQYGQQYGQQNDQQFSQQYA
PPPGPPPMAYNRPVYPPPQFQQEQAKAQLSNGYNNPNVNASNMYGPPQNMSLPPPQTQTI
QGTDQPYQYSQCTGRRKALIIGINYIGSKNQLRGCINDAHNIFNFLTNGYGYSSDDIVIL
TDDQNDLVRVPTRANMIRAMQWLVKDAQPNDSLFLHYSGHGGQTEDLDGDEEDGMDDVIY
PVDFETQGPIIDDEMHDIMVKPLQQGVRLTALFDSCHSGTVLDLPYTYSTKGIIKEPNIW
KDVGQDGLQAAISYATGNRAALIGSLGSIFKTVKGGMGNNVDRERVRQIKFSAADVVMLS
GSKDNQTSADAVEDGQNTGAMSHAFIKVMTLQPQQSYLSLLQNMRKELAGKYSQKPQLSS
SHPIDVNLQFIM [Saccharomyces cerevisiae]
Targeted Disease Leishmaniasis
Drug Resistance Mutations
Mutation info Missense: N164D [3]
References
REF 1 CRISPR-Cas9-Mediated Genome Editing in Leishmania donovani. MBio. 2015 Jul 21;6(4):e00861.
REF 2 Laboratory confirmed miltefosine resistant cases of visceral leishmaniasis from India. Parasit Vectors. 2017 Jan 31;10(1):49.
REF 3 Functional disruption of yeast metacaspase, Mca1, leads to miltefosine resistance and inability to mediate miltefosine-induced apoptotic effects.Fungal Genet Biol.2014 Jun;67:71-81.

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